Rafik Karaman

Rafik Karaman
  • Distinguished Professor (PhD)
  • Professor at Al-Quds University

1-Design, Synthesis and Bioavailability of Dopamine prodrugs. 2-Design, Synthesis and Bio of Gabapentin prodrugs.

About

314
Publications
2,200,410
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9,518
Citations
Introduction
Professor Rafik Karaman is currently a distinguished professor of pharmaceutical sciences. He received his Ph.D. MS and bachelor degree in Pharmacy from the Hebrew University. Professor Karaman has more than 200 peer-reviewed manuscripts and books; 150 of them were published in the recent 8 years. He is currently an editor and an editorial board member of 50 international journals in the area of pharmaceutical sciences. His research includes: 1.Design and synthesis of anti-cancer prodrugs having targeted properties determined on the linker’s type. 2.Design and synthesis of prodrugs having inefficient bioavailability (Dopamine). 3.Design and synthesis of prodrugs for masking bitter sensation of commonly used drugs. 4-Removal of pharmaceuticals from wastewater by novel adsorbents.
Current institution
Al-Quds University
Current position
  • Professor
Additional affiliations
January 2013 - October 2022
University of Basilicata
Position
  • Professor (Full)
Description
  • Removal of Pharmaceuticals from wastewater. stability of Pharmaceuticals in Wastewater. Synthesis, Characterization & In vitro Studies of Prodrugs For Commonly Used Drugs.
September 2005 - March 2021
Al-Quds University
Position
  • Professor
Description
  • Researching and Teaching
September 1990 - September 1993
University of California, Santa Barbara
Position
  • Professor (Assistant)
Description
  • Porphyrin Dimers. Synthesis and design by computational methods.
Education
September 1983 - September 1987
Hebrew University of Jerusalem
Field of study
  • Pharmaceutical & Medicinal Chemistry
September 1981 - January 1983
Hebrew University of Jerusalem
Field of study
  • Pharmaceutical Sciences
September 1977 - May 1981
Hebrew University of Jerusalem
Field of study
  • Pharmacy

Publications

Publications (314)
Article
Full-text available
Citation: Thawabteh, A.M.; Ghanem, A.W.; AbuMadi, S.; Thaher, D.; Jaghama, W.; Karaman, D.; Karaman, R. Promising Natural Remedies for Alzheimer's Disease Therapy. Molecules 2025, 30, 922. https:// Abstract: This study examines the intricacies of Alzheimer's disease (AD), its origins, and the potential advantages of various herbal extracts and natu...
Article
Full-text available
Red blood cells (RBCs) are a vital component of the body’s oxygen supply system. In addition to being pro-oxidants, they are also essential components of the body’s antioxidant defense mechanism. RBCs are susceptible to both endogenous and exogenous sources of oxidants. Oxyhemoglobin autoxidation is the primary source of endogenous RBC oxidant prod...
Article
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Citation: Thawabteh, A.M.; Ghanem, A.W.; AbuMadi, S.; Thaher, D.; Jaghama, W.; Karaman, R.; Scrano, L.; Bufo, S.A. Antibacterial Activity and Antifungal Activity of Monomeric Alkaloids. Toxins 2024, 16, 489. Abstract: Scientists are becoming alarmed by the rise in drug-resistant bacterial and fungal strains, which makes it more costly, time-consumi...
Book
This book covers key areas of chemistry and biochemistry research. The contributions by the authors include pathogenic fungi, antifungal activity, growth inhibition, moringa treatment, mononuclear bis(2-aminopyridine) zinc complex, nuclear magnetic resonance, 1H and 13C NMR spectra, aminopyridines, tetrazole hybrids, anti-oxidant agents, morpholine...
Article
Full-text available
The most prevalent chronic neurodegenerative illness in the world is Alzheimer’s disease (AD). It results in mental symptoms including behavioral abnormalities and cognitive impairment, which have a substantial financial and psychological impact on the relatives of the patients. The review discusses various pathophysiological mechanisms contributin...
Chapter
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Parkinson's disease is a neurodegenerative disorder that progresses aggressively and depletes the central nervous system of dopamine (DA). Dopamine replacement therapy has several issues, such as poor blood-brain barrier penetration and a progressive decline in treatment responsiveness. The primary components of this treatment are the initial prodr...
Chapter
Full-text available
Conventional taste masking methods including the use of sweeteners, amino acids and flavoring agents are often inadequate in masking the taste of highly bitter substances such as NSAIDs, i.e. ibuprofen, diclofenac sodium, mefenamic acid and etc., especially when these drugs are administered via the orally as syrups or solutions. The X-ray crystal s...
Article
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Background The study of plant-based medications, or phytomedicine, involves a wide spectrum of biological activi- ties. Due to the existence of secondary metabolites, herbal medicine has been used and practiced throughout history for the treatment of both acute and chronic conditions. Over the past century or so, numerous novel compounds with medic...
Preprint
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Recently, nanobodies have taken center stage in research on drug discovery and development. Several therapeutic possibilities using nanobodies are presently undergoing clinical trials and waiting for FDA approval. The goal of this study was to emphasize the potential of nanobodies as therapeutic agents by concentrating on the most recent published...
Article
Full-text available
Introduction: Pharmaceuticals are regarded as emerging contaminants in the environment. In recent years, their destiny and removal have piqued people's interest. Methods: Examine how well conventional wastewater treatment facilities and cutting-edge technologies (ultrafiltration and reverse osmosis) can remove specific pharmaceutical compounds from...
Article
Full-text available
Blue-green algae, or cyanobacteria, may be prevalent in our rivers and tap water. These minuscule bacteria can grow swiftly and form blooms in warm, nutrient-rich water. Toxins produced by cyanobacteria can pollute rivers and streams and harm the liver and nervous system in humans. This review highlights the properties of 25 toxin types produced by...
Book
This book covers key areas of pharmaceutical research. The contributions by the authors include anti-inflammatory activity, flavonoid, toxicity, herbal medicinal products, hyperlipidemic effects, hepatotoxicity, nephrotoxicity, oxidative stress, environmental pollution, haematological parameters, biochemical parameters, health hazards, Ibuprofen's...
Book
This book covers key areas of Medicine and Medical Research. The contributions by the authors include reproductive Age, method of sterilisation, internal carotid arteries, left vertebral artery, left subclavian artery, diagnostic & surgical procedures, vertebral arteries arch of aorta, menopause, relapsed clubfoot, demographic factors, ofluorescenc...
Article
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Human skin pigmentation and melanin synthesis are incredibly variable, and are impacted by genetics, UV exposure, and some drugs. Patients’ physical appearance, psychological health, and social functioning are all impacted by a sizable number of skin conditions that cause pigmentary abnormalities. Hyperpigmentation, where pigment appears to overflo...
Book
Chemoprevention is a new approach that employs natural plant and herbal products to prevent, delay, or even halt the progression of cancer, which is the second most common cause of death after cardiovascular disease and a major cause of mortality in affluent nations. In the pursuit of anti-neoplastic effects, traditional plant remedies are often co...
Cover Page
Full-text available
Invitation for manuscript submission to the special issue "Breakthroughs and Challenges in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes", molecules, MDPI. Submission Deadline: 31 August 2023.
Preprint
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Humans have extremely variable skin pigmentation and melanin production influenced by genetics, UV exposure, and some medications. A significant number of skin illnesses that result in pigmentary abnormalities have an impact on patients’ physical appearance as well as their psychological and social well-being. Skin pigmentation can be divided into...
Article
Full-text available
Obesity is a complex metabolic condition that can have a negative impact on one’s health and even result in mortality. The management of obesity has been addressed in a number of ways, including lifestyle changes, medication using appetite suppressants and thermogenics, and bariatric surgery for individuals who are severely obese. Liraglutide and s...
Article
Full-text available
The necessity for the discovery of innovative antimicrobials to treat life-threatening diseases has increased as multidrug-resistant bacteria has spread. Due to antibiotics' availability over the counter in many nations, antibiotic resistance is linked to overuse, abuse, and misuse of these drugs. The World Health Organization (WHO) recognized 12 f...
Book
This book covers key areas of Disease and Health Research. The contributions by the authors include acute respiratory distress syndrome, endotheliopathy, macrothrombosis, microthrombosis, multiorgan dysfunction syndrome, urinary tract infection, clinical and laboratory profile, pyuria, culture and sensitivity, serum zinc level, persistent diarrh...
Article
Full-text available
To combat the ineffectiveness of currently available pharmaceutical medications, caused by the emergence of increasingly resistant bacterial and fungal strains, novel antibacterial and anti-fungal medications are urgently needed. Novel natural compounds with antimicrobial activities can be obtained by exploring underexplored habitats such as the wo...
Article
Full-text available
SARS-CoV-2, the coronavirus disease-2019 (COVID-19), and the cause of the pandemic is extremely contagious among people and has spread around the world. Antivirals, immunomodulators, and other medications, such as antibiotics, stem cells, and plasma therapy, have all been utilized in the treatment of COVID-19. To better understand the clinical effi...
Article
Full-text available
In Mediterranean cuisine and culture, olive oil and olive fruits play a significant role. Many people believe that those who consume olive oil and its fruit live longer and have a decreased risk of illness. Olive leaves were used to treat a range of diseases in ancient times, including malaria fever and lower earaches. Although it was not understoo...
Article
Full-text available
Multiple sclerosis (MS) is known as an autoimmune disease that damages the neurons in the central nervous system. MS is characterized by its most common symptoms of spasticity, muscle spasms, neuropathic pain, tremors, bladder dysfunction, dysarthria, and some intellectual problems, including memory disturbances. Several clinical studies have been...
Book
This book covers key areas of Medicine and Medical Research. The contributions by the authors include Extranodal, Rosai Dorfman disease, histiocytic condition, Thymidine kinase 1, STK1p, health screening, meta-analysis, Pneumatisation, frontal sinus, craniofacial structures, X-Ray, Axillary mercury-in-glass thermometer, forehead non-touch infra-red...
Article
Full-text available
In this work, the stability of imidacloprid in fresh water and sludge was studied. The results revealed that the pesticide is unstable in both media. In fresh water, it underwent hydrolysis whereas a degradation to several metabolites has been observed in sludge. The rate constants for the hydrolysis and degradation at 25°C were 0.0.0067 and 0.0.00...
Book
his book covers key areas of Pharmaceutical Research and Development. The contributions by the authors include nanotechnology, nanomedicine, nanostructured lipid carriers, drug delivery, retinal pigment epithelium, pharmacotherapeutic approach, foetal health, Oncology, biotechnological advancements, therapy, urinogenital infection, therapeutic pote...
Chapter
Full-text available
Based on DFT, MP2, and hybrid GGA: MPW1k calculations for an acid-catalyzed hydrolysis of nine Kirby’s N-alkylmaleamic acids, a number of atenolol prodrugs were designed. A linear correlation of the calculated and experimental rate values for the nine Kirby’s N-alkylmaleamic acids has established credible basis for designing atenolol prodrugs that...
Article
Full-text available
Abstract: Enzymes are highly specific biological catalysts that accelerate the rate of chemical reactions within the cell. Our knowledge of how enzymes work remains incomplete. Computational methodologies such as molecular mechanics (MM) and quantum mechanical (QM) methods play an important role in elucidating the detailed mechanisms of enzymatic r...
Book
This book covers key areas of medicine and medical research. The contributions by the authors include type 2 diabetes mellitus, cardiomyopathy, oxidative stress, norepinephrine, endoplasmic reticulum stress, unfolded protein response, varicocele testis model, liver transplantation, canine model, intermediate filaments, cytoskeleton, hepatocytes, se...
Article
Full-text available
Imagination is more important than knowledge when knowledge is limited and cannot solve important questions. Inventiveness in the drug design has been clumsiness in quality and quantity. This may be due to the ineptness and incapability of medicinal chemists to comprehend biochemistry and biology issues. On the other hand, biochemists, biologists,...
Article
Full-text available
Citation: Breijyeh, Z.; Jubeh, B.; Bufo, S.A.; Karaman, R.; Scrano, L. Cannabis: A Toxin-Producing Plant with Potential Therapeutic Uses. Toxins 2021, 13, 117. https://doi.
Chapter
Full-text available
The removal efficiency of either clay (montmorillonite) or micelle-clay complex towards Cr(VI) in aqueous solutions was investigated. The micelle-clay complex was prepared from the adsorption of critical micelle concentration of octadecyltrimethylammonium ions onto clay. Batch experiments were conducted to investigate the effects of pH, contact tim...
Article
Full-text available
Alzheimer's disease (AD) is a disorder that causes degeneration of the cells in the brain and it is the main cause of dementia, which is characterized by a decline in thinking and independence in personal daily activities. AD is considered a multifactorial disease: two main hypotheses were proposed as a cause for AD, cholinergic and amyloid hypothe...
Article
Full-text available
Safflower is a Mediterranean-subtropical oil crop and has certain production potential in regions with Mediterranean climates. To assess the suitability of safflower cultivation under Palestinian climate, 56 safflower landraces were collected from different Palestinian geographical regions, and then grown in the field in two successive years (2014...
Article
Full-text available
The discovery of antibiotics has created a turning point in medical interventions to pathogenic infections, but unfortunately, each discovery was consistently followed by the emergence of resistance. The rise of multidrug-resistant bacteria has generated a great challenge to treat infections caused by bacteria with the available antibiotics. Today,...
Cover Page
Full-text available
Interests: design and synthesis of anti-cancer prodrugs having targeting properties determined by the linker's type; design and synthesis of prodrugs having inefficient bioavailability; design and synthesis of prodrugs for masking bitter sensation of commonly used drugs Special Issues and Collections in MDPI journals Special Issue Information Dear...
Article
Full-text available
Commercial non-steroidal anti-inflammatory drugs (NSAIDs) are considered as toxic to the environment since they induce side effects when consumed by humans or aquatic life. Ibuprofen is a member of the NSAID family and is widely used as an anti-inflammatory and painkiller agent.Photolysis is a potentially important method of degradation for several...
Article
Full-text available
Bacterial resistance to present antibiotics is emerging at a high pace that makes the development of new treatments a must. At the same time, the development of novel antibiotics for resistant bacteria is a slow-paced process. Amid the massive need for new drug treatments to combat resistance, time and effort preserving approaches, like the prodrug...
Article
Full-text available
Antimicrobial resistance represents an enormous global health crisis and one of the most serious threats humans face today. Some bacterial strains have acquired resistance to nearly all antibiotics. Therefore, new antibacterial agents are crucially needed to overcome resistant bacteria. In 2017, the World Health Organization (WHO) has published a l...
Article
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Background: The design and development of prodrugs is the most common and effective strategy to overcome pharmacokinetic and pharmacodynamic drawbacks of active drugs. A respected number of prodrugs have been reached the drugs market throughout history and the recent years have witnessed a significant increase in the use of prodrugs as a replaceme...
Chapter
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Non-steroidal anti-inflammatory drugs (NSAIDs) are considered as the best treatment for conditions associated with pain, fever and inflammation. Non-steroidal anti-inflammatory drugs exert their therapeutic effects by blocking prostaglandin synthesis from arachidonic acid, which inhibits the activity of cyclooxygenases (COX-1 and COX-2). COX-1 is l...
Article
Full-text available
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of Editorials that is published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal Molecules [...]
Article
Full-text available
The effluent of secondary treatment process at Al-Quds University wastewater treatment plant was tertiary treated using an Epuvalisation technique in which geranium plants (Pelargonium hortorum) was employed as a treatment vehicle. The Epuvalisation system was installed in a greenhouse in which germanium was planted hydroponically in a closed-loop...
Article
Full-text available
The growing incidence of microorganisms that resist antimicrobials is a constant concern for the scientific community, while the development of new antimicrobials from new chemical entities has become more and more expensive, time-consuming, and exacerbated by emerging drug-resistant strains. In this regard, many scientists are conducting research...
Chapter
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Prodrug design can be used in the following cases: improving active drug solubility and consequently bioavailability, increasing permeability and absorption and modifying the drug's distribution profile. In the prodrug design, a computational approach consisting of calculations using Molecular Orbital (MO) and Molecular Mechanics (MM) methods and c...
Chapter
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When knowledge fails to provide answers to important questions such as how to improve the bioavailability of vital medications, "Imagination is more important than knowledge," as Albert Einstein once said. Ingenuity in the design of effective prodrugs has been lacking in quantity and quality. The reasons behind the low quality of ingenuity could be...
Chapter
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The accumulation of knowledge on intramolecular processes, enzymes and transporters along with the vast progress in molecular revolution have accelerated the search for prodrugs having the capability to replace their corresponding current marketed drugs and to provide therapeutics with better pharmacological profiles. Utilizing the different availa...
Chapter
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This review discusses the different biological barriers that affect the delivery of therapeutic agents through membranes, such as intestinal mucosa, Brain Blood Barrier (BBB), and mediators of transport such as efflux transporters and the approaches for overcoming such barriers. The approaches illustrated in this review include: utilizing natural o...
Chapter
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Prodrug is a term used to define a pharmacologically inactive chemical entity that can be used to temporarily alter the physicochemical properties of a drug to increase its usefulness and decrease its associated toxicity. According to the definition, the inactive prodrug converts to its active parent drug and a non-toxic linker upon exposure to a p...
Article
Full-text available
In this study, the herbicide MCPA sodium salt monohydrate (sodium (4-chloro-2 methylphenoxy) acetate has been studied as are presentative compound used in the agricultural field. Accordingly, direct photolysis and photocatalytic experiments under artificial irradiation simulating solar light in laboratorial conditions were performed. Photocatalytic...
Chapter
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The focus of traditional prodrug approach was on altering various physiochemical parameters, whereas the current modern computational approach considers designing prodrugs through attaching appropriate linkers with drugs having poor bioavailability which upon exposure to physiological environments release the parent active drugs in a programmable (...
Article
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This study examines the photocatalytic activity of titanium dioxide (TiO2) semiconductor supported on borosilicate tubes (cut-off 290 nm) towards removal of a mix of persistent organic pollutants (POPs) from water. For this purpose, two widely used analgesic and anti-inflammatory drugs (NSAIDs), ibuprofen (IBU) and mefenamic acid, along with MCPA s...
Article
Full-text available
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of Editorials which is published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal Molecules [...]
Article
Full-text available
The secondary treated effluent (STE) of biological treatment process of Al-Quds University wastewater treatment plant was utilized to irrigate rosemary (Rosmarinus officinalis) using an Epuvalisation system. The Epuvalisation technology is a hydroponic treatment system in which the roots of high value crops are used to polish secondary treated wast...
Article
Introduction: Ample efforts have been carried out to improve the efficacy of a variety of drugs. The prodrugs approach was found to be a safe haven for providing medications with improved pharmacokinetic and pharmacodynamic properties. Areas covered: Herein, several selected successful prodrugs are reported and categorized. These include prodrugs f...
Article
Full-text available
In this study, the herbicide MCPA sodium salt monohydrate (sodium (4-chloro-2 methylphenoxy) acetate has been studied as are presentative compound used in the agricultural field. Accordingly, direct photolysis and photocatalytic experiments under artificial irradiation simulating solar light in laboratorial conditions were performed. Photocatalytic...
Article
Full-text available
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of Editorials, which is published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal Molecules. [...]
Article
Full-text available
A respected number of drugs suffer from bitter taste which results in patient incompliance. With the aim of solving the bitterness of guaifenesin, dimethyl maleate, maleate, glutarate, succinate and dimethyl succinate prodrugs were designed and synthesized. Molecular orbital methods were utilized for the design of the ester prodrugs. The density fu...
Article
In this study, the removal of selected pharmaceuticals including ibuprofen, diclofenac sodium, indomethacin, chlorpheniramine maleate, and paracetamol from water using natural Jordanian zeolite was studied. The influence of pH, contact time, adsorbent dosage, and initial pharmaceutical concentration on the adsorption process was investigated using...
Article
Full-text available
Background: The blood brain barrier (BBB) is a dynamic and functional structure which poses a vast challenge in the development of drugs acting on the central nervous system (CNS). While most substances are denied BBB crossing, selective penetration of substances mainly occurs through diffusion, carrier mediated transport, or receptor mediated tran...
Article
Full-text available
This study examines the photocatalytic activity of titanium dioxide (TiO 2) semiconductor supported on borosilicate tubes (cut-off 290 nm) towards removal of a mix of persistent organic pollutants (POPs) from water. For this purpose, two widely used analgesic and anti-inflammatory drugs (NSAIDs), ibuprofen (IBU) and mefenamic acid, along with MCPA...
Article
Full-text available
Paracetamol poisoning is among the most common causes of medication related poisoning and death. The evidence for all interventions for paracetamol overdose is weak. Activated charcoal, gastric lavage, and ipecacuanha are able to reduce absorption of paracetamol if started within one to two hours of paracetamol ingestion, but the clinical benefit i...
Article
Full-text available
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of Editorials, which are published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal Molecules [...]
Article
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of Editorials, which is published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal Molecules. In these Editorials, we highlight in brief reports (of about one hundred words) a number of recently published ar...
Article
Full-text available
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of Editorials, which is published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal Molecules. In these Editorials, we highlight in brief reports (of about one hundred words) a number of recently published ar...
Article
Full-text available
Background: Parkinson's disease is an aggressive and progressive neurodegenerative disorder that depletes dopamine (DA) in the central nervous system. Dopamine replacement therapy, mainly through actual dopamine and its original prodrug l-dopa (LD), faces many challenges such as poor blood brain barrier penetration and decreased response to therapy...
Article
Full-text available
Background: Poor pharmacokinetic profiles and resistance are the main two drawbacks from which currently used antiviral agents suffer, thus make them excellent targets for research, especially in the presence of viral pandemics such as HIV and hepatitis C. Methods: The strategies employed in the studies covered in this review were sorted by the typ...
Article
Full-text available
The Editorial Board of the Medicinal Chemistry section of the journal Molecules publishes here its first Editorial, which has been prepared by highlighting, in sub-editorials of about one hundred words, some selected recently published articles that may have a profound impact on drug discovery and therapy.[...]
Article
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T he reverse osmosis (RO) brine generated from the Al-Quds University wastewater treatment plant was treated using an epuvalisation system. The advanced integrated wastewater treatment plant included an activated sludge unit, two consecutive ultrafiltration (UF) membrane filters (20 kD and 100 kD cutoffs) followed by an activated carbon filter and...
Article
Background: Intensive efforts have been implemented to improve the efficacy of platinum complexes especially with emerging cisplatin resistance and elevated cancer deaths. Platinum(IV) agents show better pharmacokinetics and decreased side effects compared to Platinum(II) agents. Methods: This review aims to summarize and categorize the strategi...
Book
Adsorption of toxins and release of pharmaceuticals, are of large concern in industrial applications. In animal breading adsorbent are used for detoxification of feed from many toxicant substances produced by bacteria and fungi that can contaminate raw materials used for feed preparations. At the same time, slow release formulations of pharmaceutic...
Book
Full-text available
Adsorption of toxins and release of pharmaceuticals, are of large concern in industrial applications. In animal breading adsorbent are used for detoxification of feed from many toxicant substances produced by bacteria and fungi that can contaminate raw materials used for feed preparations. At the same time, slow release formulations of pharmaceutic...
Article
Full-text available
The occurrence, fate and effects of Pharmaceuticals compounds (PhCs) in the environmental system have been attracted special attention in the world as a new emerging contaminants due to their potential impact on humans, animals and microorganisms even at low concentrations. Conventional wastewater treatment technologies, including biological, therm...
Article
Full-text available
The occurrence, fate and effects of Pharmaceuticals compounds (PhCs) in the environmental system have been attracted special attention in the world as a new emerging contaminants due to their potential impact on humans, animals and microorganisms even at low concentrations. Conventional wastewater treatment technologies, including biological, therm...
Article
Kinetic studies on the stability of the pain killer paracetamol in Al-Quds activated sludge demonstrated that paracetamol underwent biodegradation within less than one month to furnish p-aminophenol in high yields. Characterizations of bacteria contained in Al-Quds sludge were accomplished. It was found that Pseudomonas aeruginosa is the bacterium...
Article
Full-text available
This review provides the reader a concise overview of the different biological barriers that hinder the delivery of therapeutic agents through membranes, such as intestinal mucosa, Brain Blood Barrier (BBB), and mediators of transport such as efflux transporters and etc., and the approaches for overcoming such barriers. The approaches discussed in...
Article
Sensing potentially harmful bitter substances in the oral cavity is achieved by a group of ∼25 receptors, named TAS2Rs, which are expressed in specialized sensory cells and recognize individual but overlapping sets of bitter compounds. The receptors differ in their tuning breadths ranging from narrowly to broadly tuned receptors. One of the most br...
Article
Introduction: Utilizing the prodrug approach as a method to overcome various pharmaceutical and pharmacokinetic barriers to drug delivery is significantly accelerating and achieving successes. In contrast to the older traditional prodrugs which suffer from decreased bioavailability and a high profile of side effects, due to activation at undesired...
Chapter
G protein-coupled receptors (GPCRs) are seven transmembrane (TM) proteins that play a key role in human physiology. The GPCR superfamily comprises about 800 members, classified into several classes, with rhodopsin-like Class A being the largest and most studied thus far. A huge component of the human repertoire consists of the chemosensory GPCRs, i...
Article
Full-text available
This review supplies the reader with a detailed overview on the utilization of intramolecular processes for a design and synthesis of prodrugs. It is well known that a respected number of drugs suffer from low bioavailability, toxicity, unpleasant taste and presystemic first-pass metabolism which result in drug inactivation. The classical prodrug a...
Article
Full-text available
A number of marketed antibacterial drugs suffer several problems, such as bitter sensation and low stability which lead to patient incompliance. The prodrug approach is considered the most promising and extremely exciting method to overcome such problems. Based on our previously reported density functional theory (DFT) calculations, amoxicillin Pro...
Article
Full-text available
In this study, the stability of chlorpyrifos, a known pesticide, in fresh water and sludge was investigated. The results showed that chlorpyrifos underwent hydrolysis in both media to give two main metabolites: 3,5,6-trichoro-2-pyridiniol (TCP) and diethylthiophosphoric acid (DETP). The hydrolysis reaction in both media was found to follow first-or...
Article
Full-text available
Using DFT molecular orbital at B3LYP 6-31G (d,p) and B3LYP/311+G (d,p) levels and molecular mechanics (MM2) calculations of the hydrolysis of Bruice’s di-carboxylic semi-esters 1–5 several atovaquone prodrugs were designed. It was found that the interconversion rate of the designed atovaquone prodrugs is largely determined on the strain energies of...
Article
Full-text available
Two novel prodrugs of amoxicillin and cephalexin (amoxicillin ProD 1 and cephalexin ProD 1, respectively) were designed and synthesized to improve the stability and bitter sensation of their parent drugs. The in vitro susceptibility for both prodrugs was determined against Escherichia coli, staphylococcus epidermidis, staphylococcus aureus, Klebsie...
Article
Full-text available
The predrug (prodrug) term involves chemically modified inert compound which upon an administration releases the active parent drug to elicit its pharmacological response within the body. For many years, the predrug strategy has been extensively developed to solve many unwanted drug properties. This approach has several advantages over conventional...
Article
Full-text available
The classical approach for delivery of drugs into the central nervous system (CNS) is associated with adverse effects and it has many limitations. Therefore, extensive efforts have been done in searching and developing novel methods for achieving such delivery. This mini-review discusses the design and synthesis of selected targeting prodrugs for t...
Article
Full-text available
Stability and removal of spironolactone (SP) from wastewater produced at Al-Quds University Campus were investigated. Kinetic studies on both pure water and wastewater coming from secondary treatment (activated sludge) demonstrated that the potassiumsparing diuretic (water pill), spironolactone, underwent degradation to its hydrolytic derivative, c...
Article
Full-text available
The conventional old treatment method for cancer therapy is associated with severe side effects along with several limitations. Therefore, searching and developing new methods for cancer became crucial. This mini review was devoted on the design and synthesis of prodrugs for cancer treatment. The methods discussed include targeted prodrugs which ar...

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