Md. Jawaid Akhtar

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• M. Pharm, Ph.D.
• Professor (Assistant) at National University of Science and Technology, Oman

Coumarin (2‐benzopyrone), a secondary plant metabolite, is considered a privileged scaffold in medicinal chemistry. Coumarin and its derivatives have been demonstrated to exhibit various biological activities such as antiviral, antibacterial, anticancer, anti‐inflammatory, anticonvulsant, antioxidant, antidepressant, anti‐Alzheimer, antidepressant,...

Epidermal growth factor receptor (EGFR) mutations, especially in non‐small cell lung cancer (NSCLC), present significant challenges to targeted therapies due to acquired resistance. This study reports the synthesis and evaluation of a series of pyrimidine‐furan derivatives as potential anticancer agents. The compounds were screened using MTT and br...

The toxicity associated with synthetic drugs used for treating various diseases is common. This led to a growing interest in searching and incorporating natural functional core structures such as flavonoid and their derivatives via chemical modifications to overcome the toxicity problems and enhance their biological spectrum. Natural core structure...

A drug design strategy with reduced side effects and economic feasibility is desirable for fatal diseases. Increasing the bioavailability of a drug using a bioenhancer is a smart strategy. Herbal/natural bioenhancers with no probable side effects are an ideal choice to enhance the pharmacokinetics of a therapeutic drug synergistically. The mechanis...

Phytochemistry and Neuroprotective Spectrum of Crocus sativus Linn.

Ebola virus disease (EVD) is a rare, highly contagious and a deadly disease with a variable fatality rate ranging from 30% to 90%. Over the past two decades, Ebola pandemic has severely affected the sub-Sahara region including Democratic Republic of the Congo (DRC), and Uganda. The causative agents of the most EVD cases are three distinct species o...

Sulfur‐containing heterocyclic derivatives have been disclosed for binding with a wide range of cancer‐specific protein targets. Various interesting derivatives of sulfur‐containing heterocyclics such as benzothiazole, thiazole, thiophene, thiazolidinedione, benzothiophene, and phenothiazine, etc have been shown to inhibit diverse signaling pathway...

The demand and usage of alcohol-based hand sanitizers have immensely increased worldwide in recent times as a protective measure against COVID-19 and other infectious diseases. To ensure that the public and health workers get hand sanitizers with an alcohol percentage within the label stated range, quality control of these products must be carried...

Cancer is the world’s leading cause of death impacting millions of lives globally. The increasing research over the past several decades has focused on the development of new anticancer drugs, but still cancer continues to be a global health challenge. Thus, several new alternative therapeutic strategies have been tried for the drug design and disc...

The physicochemical properties of non-chromophoric compounds that lack a group to absorb UV-visible radiation make them difficult to analyze with a simple detector. Pharmaceutical formulations and their unknown impurities, which show weak or no response with a UV detector, remain undetected and pose a challenge to the analysis of these compounds. D...

The objective of this study was the development, optimization, and validation of a RP-HPLC method for the quantification of reduced glutathione (GSH) and oxidized glutathione (GSSG) in pharmaceutical formulations The separation utilized a C18 column at room temperature with absorption wavelength 210nm. The mobile phase was an isocratic flow of a 95...

Fourier transform infrared spectroscopy is an effectual and non-critical approach for quantitative study of different types analytes present in pharmaceutical and foodstuffs. The present review describes the basic principles and the instrumentation of FTIR spectroscopy along with its sample preparation techniques, sample handling techniques and adv...

The excessive use of antimicrobials and rapid resistance to antibiotics is a major concern for health care providers. Hence there is a need to develop effective antimicrobials. Natural sources are considered as the potential source of antimicrobial agents. The study aimed to decrease the pungency or irritancy effects of the allyl isothiocyanate (AI...

Over the years, extensive research on mustard oil has revealed the presence of isothiocyanates as pungent toxic compounds and erucic acids as possible health risks. Hence, strategies are needed to remove or reduce the isocyanates and erucic contents while processing the mustard oil. Conversely, due to the presence of monounsaturated fatty acids and...

Leishmaniasis is a parasitic disease and categorised as a neglected tropical disease (NTD). Each year, between 70,0000 and 1 million new cases are believed to occur. There are approximately 90 sandfly species which can spread the Leishmania parasites (over 20 species) causing 20,000 to 30,000 death per year. Currently, leishmaniasis has no specific...

The study aimes to investigate the physicochemical properties of seven honey samples to assess their quality as per GCC Standardization Organization (GSO) and international standard parameters. Seven honey samples, four marketed honey samples, and three locally produced Omani honey were collected and analysed for the pH, acidic content, % of insolu...

Proteolysis-targeting technology is a new emerging technique to target mutated, denatured, and misfolded proteins that accumulate in various parts of the body. The accumulation of these aggregated harmful proteins, such as β-amyloid (Aβ), tau, mHTT, polyglutamates, and other proteins in the brain, are some of the reasons for the development of neur...

Acetylcholine (ACh) neurotransmitter of the cholinergic system in the brain is involved in learning, memory, stress responses, and cognitive functioning. It is hydrolyzed into choline and acetic acid by two key cholinesterase enzymes, viz., acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). A loss or degeneration of cholinergic neurons...

Neurodegenerative disorders (NDDs) are multifaceted complex disorders that have put a great health and economic burden around the globe nowadays. The multi-factorial nature of NDDs has presented a great challenge in drug discovery and continuous efforts are in progress in search of suitable therapeutic candidates. Nature has a great wealth of activ...

Pomegranate (Punica granatum) represents a major source of polyphenolic compounds. It has been gaining importance because of varied pharmacological activities attributed to its phytochemicals. This comprehensive review aimed to provide an exhaustive list of phytoconstituents found in pomegranate fruits, peel, flowers, and seeds along with their pha...

Pregnant women and children are kept under special group of patients that needs extra efforts while selecting drug therapy for this group of patients. The use of anti-infective medicines in pregnant women and children has several limitations because of altered pharmacokinetics and pharmacodynamics of anti-infectives in these groups of patients, whi...

The sodium dependent SLC13 family transporters comprise of five genes SLC13A1, SLC13A2 (NaDC1), SLC13A3 (NaDC3), SLC13A4 and SLC13A5 (NaCT). Among them, NaDC1, NaDC3 and NaCT are sodium dependent transporters belonging to family of dicarboxylates (succinate, malate, α-ketoglutarate) and tricarboxylates (citrate). The mouse and the human NaCT struct...

s According to the WHO’s data for 2018, the global cancer burden was estimated to have risen to 18.1 million new cases and which alone accounted for 9.6 million deaths. Cancer is a group of diseases known as tumors that often spreads throughout the body, and may cause harm to multiple organs in the body. The global pharmaceutical spending is around...

Ayurvedic Medicine, or Ayurveda, is a traditional Indian health care system. Research into the medicinal plants utilised in Ayurveda is becoming a global endeavour, and large pharmaceutical companies are investing in novel drug discovery from Ayurvedic sources as a number of clinical studies have demonstrated efficacy of natural products from Ayurv...

The sodium dependent SLC13 family transporters comprise of the five genes SLC13A1, SLC13A2 (NaDC1), SLC13A3 (NaDC3), SLC13A4 and SLC13A5 (NaCT). Among them the three NaDC1, NaDC3 and NaCT are sodium dependent transporters such as di-carboxylates (succinate, malate, α-ketoglutarate) and tricarboxylates (citrate). The mouse and the human NaCT structu...

Chlorpyrifos (CP) and its highly electrophilic intermediates are principal toxic metabolites. The active form of CP i.e. chlorpyrifos oxon (CP-oxon) is responsible for both the insecticidal activity and is also of greater risk when present in the atmosphere. Thus, the combined effects of both CP, CP-oxan, and other metabolites enhance our understan...

Alzheimer’s disease (AD) is a neurological disorder that leads to dementia i.e., progressive memory loss accompanied with worsening of thinking ability of an individual. The cause of AD is not fully understood but it progresses with age where brain cells gradually die over time. According to WHO, currently 50 million people worldwide are affected b...

A series of new clubbed aryl oxadiazole-1,2,4-triazine derivatives (6a-l) were designed and synthesized using appropriate chemical routes. The structures were designed to have the required structural elements for any compounds to be potential anticonvulsant. Preliminary screening of anticonvulsant activity was performed using maximal electroshock s...

Gamma-Aminobutyric Acid (GABA) inhibitory neurotransmitter departs an energetic role in brain signalling system. Levels of GABA in the brain influence human behaviour, diminishes in the degree of GABA can cause seizures, depression, Parkinson's. To put it plainly, it plays a basic part in the significant issues of mind. It is exceptionally importan...

Introduction Alzheimer’s disease (AD) is one of the most common and prevalent forms of neurodegenerative diseases. Coumarin is a versatile scaffold that exhibits a wide range of biological properties including cholinesterase inhibitory activity and therefore is an important heterocyclic moiety to develop anti-AD drugs. Objectives This study aimed...

The new series of N-(5,6-diphenyl-1,2,4-triazin-3-yl)-2-(4-substituted piperazin-1-yl) acetamide (RP1-5) and 2-((5,6-diphenyl-1,2,4-triazin-3-yl)thio)-1-(4- substituted piperazin-1-yl)-ethan-1-one (RP6-10) derivatives were designed and synthesised by clubbing substituted 5,6-diphenyl-1,2,4-triazine with different substituted piperazines. The synthe...

A series of new clubbed aryl oxadiazole-1,2,4-triazine derivatives (6a-l) were designed and synthesized using appropriate chemical routes. The structures were designed having the required structural elements for any compounds to be potential anticonvulsant. Preliminary (Phase I) screening of anticonvulsant activity was performed by means of maximal...

Doxorubicin belongs to the anthracycline chemical class of the drug and is one of the widely used anticancer drugs. The common side effects of doxorubicin include vomiting, hair loss, rashes to serious side-effects such as irreversible cardiotoxicity, and drug-induced leukemia. This led many researchers around the globe to develop methods aimed to...

Several generations of antiepileptic drugs (AEDs) are available in the market for the treatment of sei�zures, but these are amalgamated with acute to chronic side effects. The most common side effects of AEDs are dose-related, but some are idiosyncratic adverse drug reactions (ADRs) that transpire due to the formation of reactive metabolite (RM) af...

Several generations of antiepileptic drugs (AEDs) are available in the market for the treatment of seizures, but these are amalgamated with acute to chronic side effects. The most common side effects of AEDs are dose-related, but some are idiosyncratic adverse drug reactions (ADRs) that transpire due to the formation of reactive metabolite (RM) aft...

Epilepsy is a chronic neurological disorder, characterized by predisposition of unprovoked seizures affecting the neurobiological, psychological, cognitive, economic, and social well-being of patient. As per the 2019 report by World Health Organization, it affects nearly 80% of the population which comes from the middle to low-income countries. It...

Voltage-gated sodium channel blockers are one of the vital targets for the management of several central nervous system diseases, including epilepsy, chronic pain, psychiatric disorders, and spasticity. The voltage-gated sodium channels play a key role in controlling cellular excitability. This reduction in excitotoxicity is also applied to improve...

Background Hydroxychloroquine (HCQ) was initially launched as an antimalarial drug, but now it is also used as a slow-acting anti-rheumatic drug. It contains equal proportions of (-)-(R)-hydroxychloroquine and (+)-(S)-hydroxychloroquine. Introduction Hydroxychloroquine, a synthetic 4-aminoquinoline derivative, possesses antimalarial, antirheumatic...

Alzheimer's disease (AD) is a major progressive and perplexing cortical degenerative disease of the brain in the elderly. It contributes to a significant socio-economic burden on patients, families, and care providers in comparison to cancer, cardiovascular diseases, and stroke in general. Recently, a hybridized approach based on multi-target direc...

The study aimed to characterize the volatile constituents of Mentha spicata L., grown in Oman, and to investigate in vitro cytotoxic and antioxidant activities of the volatile oil. The pale-yellow color essential oil (% yield 0.55% v/w) showed the presence of thirteen compounds representing 99.19% of the total constituents. d-Carvone (65.21%) and d...

Depression is the single largest contributor to global disability with a huge economic and social burden on the world. There are a number of antidepressant drugs on the market, but treatment‐resistant depression and relapse of depression in a large number of patients have increased problems for clinicians. One peculiarity observed in most of the ma...

A series of N-(substituted benzothiazole-2-yl)-2-(2,3-dioxoindolin-1-yl)acetamide (4a-i) and substituted-[3-((5-phenyl-1,3,4-oxadiazole-2-yl)imino)indolene-2-one] (5a-f) were designed, synthesized fulfilling the structural requirement of pharmacophore and evaluated for anticonvulsant activities using maximal electroshock test (MES), subcutaneous pe...

According to the World Health Organization (WHO), depression is a common mental disorder and includes complex interaction between social and psychological behaviour affecting 264 million people worldwide. The review aims to highlight the role and importance of nitrogen-based heterocyclics in the development of antidepressant compounds. Many researc...

Schiff base or imine or azomethine is one of the most important organic compounds that has been reported to play a significant role in various biological processes. The group is a part of natural or non-natural compounds and is involved as important precursors as diversified agents and as intermediates for the synthesis of biologically active agent...

Epilepsy is one of the commonly prevailing neurological disorders. According to the reports, it is evident that about 80% of the epileptic cases have been observed in developing countries. Although there are many drugs with significant potency available in the market; still there is an issue of selectivity and toxicity. Therefore, continuous attemp...

The inhibition of viral targets might provide new therapies for coronavirus disease abbreviated as COVID-19. The rational drug design identified as much of the recent discoveries of potent drugs molecule against any targets. This results in an improvement in bindings for better potency and selectivity. The drugs containing ethanolamine/propylamine...

The increase in psychiatric and neurological disorders includes Parkinson's, Schizophrenia, Alzheimer's and Depression over the last 50 years adds concerns to society. In contrast, there have been great advances in elucidating the receptors of CNS and their interaction with the novel molecules. Enzymes inhibitors are on the top plan to interact spe...

This review presented the detailed account of factors leading to cancer and design strategy for the synthesis of benzimidazole derivatives as anticancer agents. The recent survey for cancer treatment in Cancer facts and figures 2017 American Chemical society has shown progressive development in fighting cancer. Researchers all over the world in bot...

The original version of this article unfortunately contained a mistake in university name of Sharique Ahmed.

A series of 9-(2-(1-arylethylidene)hydrazinyl)acridine and its analogs were designed, synthesized and evaluated for biological activities. Various biochemical assays were performed to determine the free radical scavenging capacity of synthesized compounds (4a–4j). Anticancer activity of these compounds was assessed against two different human cance...

Alzheimer, the fourth leading cause of death embodies a key responsible event including formation of β-amyloid protein clustering to amyloid plaque on blood vessels. The origin of above events is Amyloid precursor protein (APP) which is an integral membrane protein known for its function in synapses formation. Modern research had proposed that the...

Diabetes has turned out to be an epidemic in the recent years all over the world, and today it has become a burden on the healthcare system. Over the years, with technological advancements, different classes of antidiabetic medications have emerged, like sulfonylureas, biguanides, alpha‐glucosidase inhibitors, and thiazolidinediones, but these are...

The study performed molecular docking, formulated, characterized thymoquinone (TQ) loaded solid lipid nano particles (TQSLN) and exhibited comparative antidepressant activity. TQ loaded nano lipid formulations were prepared by solvent injection methods and characterize for different in-vitro parameters. The optimized formulation was evaluated for d...

Quinazoline is a heterocyclic compound having biological activities. It is aromatic in nature having bicyclic structure containing benzene ring and pyrimidine ring. Quinazoline and its derivatives are found to have wide range of biological activities that is anticancer, analgesic, antimicrobial, antihypertensive, anticonvulsant, antimalarial, antit...

A new series of benzimidazole linked pyrazole derivatives were synthesized by cyclocondensation reaction through one-pot multicomponent reaction in absolute ethanol. All the synthesized compounds were tested for their in vitro anticancer activities on five human cancer cell lines including MCF-7, HaCaT, MDA-MB231, A549 and HepG2. EGFR receptor inhi...

Metabolic disorders are closely associated with dietary habits and seem to be related to neuroinflammation and neurodegenerative disease in humans. Emblica officinalis (EOT) fruits not only have good nutritional value but also have excellent therapeutic potential. We used a tannins-enriched fraction of EOT fruit with the expectation of controlling...

A series of new hybrid benzothiazole containing pyridazinones derivatives were designed and synthesized fulfilling all the pharmacophoric requirements essential for the anticonvulsant activity. In-silico and in vitro studies revealed that some of these hybrid derivatives demonstrated admirable GABA AT inhibitory activity. An attempt has also been m...

The synthesis of benzimidazole linked oxadiazole derivatives designed as potential EGFR and erbB2 receptor inhibitors with anticancer and apoptotic activity were studied. Compounds 7a specifically inhibit EGFR and erbB2 receptor at 0.081 and 0.098 μM concentration. Some of the compounds showed strong, broad-spectrum antiproliferative activitiy when...

A series of new hybrid benzimidazole containing pyridazinones derivatives were designed and synthesized in accordance with the pharmacophoric requirements essential for the anticonvulsant activity. The synthesized compounds were evaluated for anticonvulsant activity on mice by the gold standard maximal electroshock (MES) and subcutaneous pentylenet...

Recent attention is focused on the impact of diet on health and mental well-being. High-salt and cholesterol diet (HSCD) is known to be associated with neuroinflammation which is the predominant factor for neurodegenerative disease like Alzheimer disease (AD). In the present study, we examined the neuroprotective potential of rosuvastatin, an HMG-C...

New N3-benzylidene (substituted)-2-phenyl-N4-(thiazol-2-yl)-quinazoline-3,4-(4H)-diamine derivatives were design and synthesized by a sequence of reactions starting from appropriate 6-methyl anthranilic acid. The title compounds were screened for in vitro dipeptidyl peptidase IV (DPP-4) inhibitory activity and diphenyl-2-picryl-hydrazyl (DPPH) assa...

A novel series of quinazoline clubbed thiazoline derivatives was rationally designed and synthesized. The newly synthesized compounds were evaluated for in vitro dipeptidyl peptidase IV (DPP-4) inhibitory activity. Compounds that showed good to moderate activity were compared using linagliptin as standard. Compound 4x (IC50 = 1.12 nM) exhibited the...

Objective: The present review article presented a detailed account of the design strategies and the structure activity relationship of different derivatives apart from the nitrogen containing ring. These scaffolds play an important part in the drug discovery which showed anticancer activity against different human cancer cell lines through apoptos...

The present review article offers a detailed account of the design strategies employed for the synthesis of nitrogen-containing anticancer agents. The results of different studies describe the N-heterocyclic ring system is a core structure in many synthetic compounds exhibiting a broad range of biological activities. Benzimidazole, benzothiazole, i...

As per structural requirement essential for anticonvulsant activity, a series of new 6-(2-amino-substituted phenyl)-4-(substituted phenyl)-1,2,4-triazine-3,5-dione derivatives were designed and synthesized. All the synthesized title derivatives were assessed for in vivo anticonvulsant screening by the two most employed standard animal seizure model...

A series of 3-(4-substitutedphenyl)-N-(5-(4-substitutedphenyl-1,3,4-oxadiazol-2-yl)but-2-enamide were synthesized using pharmacophoric elements for in vivo anticonvulsant activity yielding two potent candidates (4d and 4j) in the Phase I and Phase II screening employing maximal electroshock seizure and subcutaneous pentylenetetrazole test having mi...

The use of current antiepileptic drugs has been questioned due to the nonselectivity of the drugs and the undesirable side effects posed by them. This led to an intensive investigation in this area worldwide during the past 10 years. There have been some significant outcomes and the findings are promising as far as drug efficacy and safety is conce...

Synthesis Of Novel Substituted Benzimidazole Derivatives As Potential Antimicrobial Agents

A large and emergent demand for the pyridine derivatives exists because of their many medicinal, pharmaceutical and agricultural uses. The pyridine derivatives have several considerable biological applications such as anticonvulsant, antimicrobial, antidiabetic, antiviral, anticancer and antimycobacterial agents. Potential novel routes include the...

Triazoles and its derivatives possess a great importance in medicinal chemistry and can be used for the synthesis of numerous heterocyclic compounds with different biological activities. This review article covers the latest information over active triazoles derivatives having different pharmacological action such as, antiviral, antibacterial, anti...

Depression is currently the fourth leading cause of disease or disability worldwide. Antidepressant is approved for the treatment of major depression (including paediatric depression), obsessive-compulsive disorder (in both adult and paediatric populations), bulimia nervosa, panic disorder and premenstrual dysphoric disorder. Antidepressant is a ps...