Rafik Karaman

Al-Quds University · Faculty of Pharmacy

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...

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...

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...

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...

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...

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...

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...

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,...

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.

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...

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...

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...

Breakthroughs in Medicinal Chemistry [...]

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,...

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...

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...

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...

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...

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...

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...

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 [...]

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...

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...

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...

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...

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...

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...

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...

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...

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 (...

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...

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 [...]

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...

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...

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...

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. [...]

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...

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...

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...

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...

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...

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 [...]

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...

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...

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...

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...

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.[...]

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...

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...