Mohammad Shahar Yar

• M Pharm, PhD
• Professor at Jamia Hamdard

Pyrazoline is a 5-membered ring that has two adjacent nitrogen. It has gained advanced attention from medical and organic chemists due to very low cytotoxic activities. It is applicable and more applied in research fields and has various pharmacological activities, including cardiovascular, anti-tumor, and anti-cancer properties. In this review, th...

Lavandula stoechas L., also referred to as French lavender or Spanish lavender, is a well‐known medicinal plant with a strong presence in traditional medicine systems. This review provides an overview of the existing research progress on L. stoechas, encompassing its traditional uses, medicinal phytochemistry, pharmacological activity as well as cl...

Dipeptidyl peptidase‐4 (DPP4) inhibitors are promising therapeutic targets for the treatment of a catastrophic disease, especially diabetes mellitus (DM), which contributed to a massive rate of mortality. This research work succinctly covers the significance and vital role of gliptins in diabetes management and in the potential areas of further ant...

The Pummerer rearrangement is extensively utilized for the preparation of various heterocyclic compounds, as well as for the introduction of functional groups such as carbonyl, hydroxyl, and amino groups into organic molecules. The reaction mechanism typically proceeds through an initial electrophilic attack by Lewis acid or another electrophile on...

The synthesis of 3,5-disubstituted pyrazolines, integrated with heterocyclic systems, represents a crucial area of chemical research due to their pharmacological and biological significance. This article reviews various synthetic methods used to prepare 3,5-disubstituted pyrazolines with different heterocyclic groups. The methodology employed in th...

Cancer has been the cause of the highest number of deaths in the human population despite the development and advancement in treatment therapies. The toxicity, drug resistance, and side effects of the current medicaments and therapies have left the void for more research and development. One of the possibilities to fill this void is by incorporatin...

The intricate nature of Alzheimer’s disease (AD) has presented significant hurdles in the development of effective interventions. Sulforaphane (SFN) is of interest due to its antioxidative, anti-inflammatory, and neuroprotective properties, which could address various aspects of AD pathology. This study explores the potential of SFN in a rat model...

Dipeptidyl peptidase 4 (DPP-4), well known as the T-cell antigen CD26 enzyme which, was discovered in the year of 1966 by Hopsu-Havu and Glenner. The enzyme gained considerable attention due to its vital functions, such as (1) deactivation of the incretin hormone, which is responsible for insulin catabolism, (2) hydrolyzes of opioid peptides engage...

Pyrazolines are preferred to be stable heterocycles in medication development. It has been established from previous research that the 2‐pyrazolone scaffold is a common pattern that can be found in many pharmacologically significant therapeutic compounds. They are said to have a wide range of biological actions and have been thoroughly investigated...

Aim/Background: Novel quinoline compounds containing benzimidazole have been synthesized in a number of different ways and screened for anti-epileptic potential through in vivo and in silico studies. Materials and Methods: The novel quinoline-benzimidazole hybrids were synthesized by using substituted carbaldehyde (1,2) and substituted benzimidazol...

Topiramate, a second-generation antiepileptic drug used to manage and treat epileptic seizures was approved by the FDA in 1996 as a solo or supplementary for the therapy of epilepsy. The frequency, severity, quality of life, and adverse events that topiramate has on epilepsy patients, including children and adolescents, are summarized in this revie...

Background: Two significant families of compounds i.e. 1,3,4-oxadiazole and ben-zimidazole, have undergone extensive investigation into their pharmacological characteristics and possible therapeutic applications. Both classes have shown their potential in a variety of ap-plications, and because of their synergistic interactions, they may have an ev...

Oxadiazoles and thiadiazoles are malleable heterocycles that have recently generated major interest in the field of medicinal chemistry. Compounds based on these moieties have versatile biological applications such as anticonvulsant, anticancer, antidiabetic, and antioxidant agents. Due to the versatile nature and stability of the oxadiazole and th...

Background Piperine is a natural compound found in black pepper that has been traditionally used for various therapeutic purposes. In the ayurvedic system of medication there is a lot of evidence which shows that the piperine is widely used for different therapeutic purpose. In recent years, there has been an increasing interest in the pharmacologi...

Hepatocellular carcinoma (HCC) is the seventh most common cancer and the third leading cause of cancer-related death globally. It has a poor prognosis and is resistant to the majority of chemotherapeutics. The present review aimed to highlight studies into the tumor cycle and its prevention by appropriate herbal (Ayurvedic/Unani) medicine that is e...

In recent eras, cancer, and tuberculosis have become the leading causes of not only morbidity but also mortality. Around 10 million cancer-related fatalities are reported annually worldwide, but 10.4 million new cases are also discovered each year. According to World Health Organization data, 10.4 million cases were in 2016 worldwide, whereas 360,5...

Hepatocellular carcinoma (HCC) is the 7th most common cancer and the 3rd leading cause of cancer-related death worldwide. It is resistant to the majority of chemotherapeutics and has a dismal prognosis. Hepatocellular carcinoma is a prevalent complication of chronic liver disease (CLD) in India. Primary liver cancer is the 6th most common cancer wo...

Nitrogen‐containing hybrid heterocyclic compounds have been gaining attention in the field of drug discovery and development due to their diverse pharmacological activities and relatively low toxicity. This study aimed to synthesize a series of new quinoline‐bearing amino acid‐derived benzimidazole derivatives i. e. 3‐{[1‐(1H‐Benzoimidazol‐2‐yl)‐su...

In the past two decades, there has been sudden development in antiepileptic drugs (AEDs) for the adjunctive treatment of epilepsy. CNB is a leading-edge new generation tetrazole-derived carbamate for the treatment of focal-onset epileptic seizures where the mode of action is mediated by blocking voltage-gated sodium channels and interaction with th...

Quinoline has recently become an important heterocyclic molecule due to its numerous industrial and synthetic organic chemistry applications. Quinoline derivatives have been used in clinical trials for a variety of medical conditions that causes cancer. The present literature study is composed of recent progress (mainly from 2010 to the present) in...

Both, benzimidazole and quinoline pharmacophores have shown various activities against cancer, tuberculosis, malaria, fungal, viral and bacterial infections. These moieties are considered highly potent nuclei in medicinal chemistry. Thus, this research work aims to produce a synergistic effect involving both nuclei in a single structure. A Series o...

Heterocyclic compounds are fundamental building blocks for developing novel bioactive compounds. Due to their extensive uses in both industrial and synthetic organic chemistry, quinoline and benzimidazole have recently become important heterocycles. Clinical trials have investigated quinoline and benzimidazole analogues to treat a variety of illnes...

Aim/Background: This research work aims to design and synthesize novel compounds containing pyrazoline moiety in their structure with enhanced anticonvulsant activity in comparison with the standard (Phenytoin) drug. In the docking study, the target protein with the active site of human mitochondrial branched-chain aminotransferase (BCATm) (PDB ID:...

In the presented manuscript, a new series of 2-[4-methoxy-3-(5-substituted phenyl-[1,3,4]oxadiazol-2-ylmethoxy)-phenyl]-benzothiazoles (6a-n) have been synthesized and studied in vivo and in silico for their anticonvulsant potential. Maximum electroshocks (MES) and subcutaneous pentylenetetrazol (scPTZ) models have been used for in vivo anticonvuls...

One of the leading causes of death worldwide is cancer, which poses substantial risks to both society and an individual's life. Cancer therapy is still challenging, despite developments in the field and continued research into cancer prevention. The search for novel anticancer active agents with a broader cytotoxicity range is therefore continuousl...

A series of new 1,2,4-triazolo-linked bis-indolyl conjugates (15a–r) were prepared by multistep synthesis and evaluated for their cytotoxic activity against various human cancer cell lines. It was observed that they were more susceptible to colon and breast cancer cells. Conjugates 15o (IC50 = 2.04 μM) and 15r (IC50 = 0.85 μM) illustrated promising...

Currently, black pepper commands the leading position among all the spices as a spice of great commercial importance in all the world trade and finds its way into the dietary habits of millions of people worldwide. Black pepper is biologically known as Piper nigrum and contains piperine as the main active chemical constituent. This paper highlights...

Background Benzimidazole (Benz-fused bicyclic ring system) is the most versatile class of heterocyclic compounds due to their numerous applications in industrial and synthetic organic chemistry because of its many biological actions. Benzimidazole analogs have been utilized to discover a variety of medical problems, such as cancer, bacterial infect...

Due to their diverse applications in industrial and synthetic organic chemistry, quinoline and 1,3,4-oxadiazole have become important heterocyclic compounds. Quinoline and 1,3,4-oxadiazole compounds have been developed for various medical conditions such as anti-cancer, anti-bacterial, anti-fungal, antimalarial, antioxidants, anti-HIV, anticonvulsa...

Heterocyclic scaffolds of natural as well as synthetic origin provide almost all categories of drugs exhibiting a wide range of pharmacological activities, such as antibiotics, antidiabetic and anticancer agents, and so on. Under normal homeostasis, aldose reductase 2 (ALR2) regulates vital metabolic functions; however, in pathological conditions l...

Objectives: CB1 antagonism arbitrates a dormant shape to the endocannabinoid system that alleviates diverse pathological incidents of diabesity. The present study pursued the synthesis and evaluation of thiazolidine derivative (BAC) having pleiotropic action on CB1R, with or without AM251 (selective antagonist of the CB1 receptor) against high-fat...

We herein report a new series of indole‐tethered pyrazoline derivatives as potent anticancer agents. A total of 12 compounds were designed and synthesized by conventional as well as microwave‐irradiated synthesis methods. The latter method results in a significant reduction in the duration of reaction along with improved yields. All synthesized der...

Purpose: The current research investigated the development and evaluation of dual drug-loaded nanostructure lipidic carriers (NLCs) of green tea extract and Ribociclib. Method: In silico study were performed to determine the effectiveness of combinational approach. The prepared NLCs were subjected to in vitro drug release, lipolysis, haemolysis...

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A new series of 2‐aminobenzothiazole derivatives was designed, synthesized and evaluated for their anticancer activity against the MCF7, MDAMB‐231, and HepG2 cancer cell lines. All synthesized derivatives (8a–8n) demonstrated moderate to high anticancer activity against the tested cell lines. As the most potent compound in the series, compound 8i d...

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...

Cancer is one of the leading causes of death globally, around 10 million deaths are reported every year due to cancer. Some clinically approved anticancer drugs play a riveting role in its treatment. Still, due to the severe emergence of drug resistance, side effects, and multidrug-resistant cancers due to mutations, it creates a significant demand...

Background Pyrazoline is a heterocyclic compound of five rings, three carbon atoms, and two nitrogen atoms in a circle with just one endocyclic bond. Pyrazoline is one form of electron-rich nitrogen carrier, gaining popularity because it combines exciting electronic properties with the potential for dynamic applications. Many methods have been used...

Cancer is one of the leading causes of death. Globally a huge number of deaths and new incidences are reported annually. Heterocyclic compounds have been proved to be very effective in the treatment of different types of cancer. Among different heterocyclic scaffolds, quinazoline and quinazolinone core were found versatile and interesting with many...

Introduction: Hyperactivated RAS signaling is reported in 13% of all human cancers, in which ~80% resulted due to KRAS mutations alone. Direct inhibition of KRAS is an important aspect in treating KRAS-related tumors. Despite the efforts of more than four decades, not many KRAS inhibitors have been successful in obtaining clinical approval, except...

Benzimidazole is one of the privileged nitrogen-containing scaffolds known for its versatile diversified role in insecticides, pesticides, dyes, pigments and pharmaceuticals. Due to its electron-rich environment, structural features and binding potency of various therapeutic targets, benzimidazole derivatives exhibit a broad spectrum of biological...

In recent times cancer has become one of the leading causes of death. Globally around 11 million deaths are reported every year due to cancer. Some clinically approved anticancer drugs play a riveting role in its treatment. Still, due to the severe emergence of drug resistance, side effect, and multidrug-resistant cancers due to mutations, the dema...

Currently, black pepper commands the leading position among all the spices as a spice of handsome commercial importance in all the world trade and finds its way into the dietary habits of millions of people worldwide. Black pepper is biologically known as Piper nigrum and contains Piperine as the main active chemical constituent. This paper highlig...

New drugs introduced on the market each year have privileged structures specifically for anticancer targets, of which quinoline-based analogues also play an important role. This review lit up quinoline and its derivatives, which have great potency against various cancer cells including prostate cancer, breast cancer, colon cancer, pancreas cancer a...

Dual TK inhibitors have shown significant clinical effects against many tumors, but with unmanageable side effects. Design approach and selectivity of these inhibitors plays substantial role in their potency and side-effects. Understanding the homology of binding sites in targeted receptors, and involvement of signaling proteins after the inhibitio...

Diabetes is a major public health problem that severely affects the quality of life of many people. The discovery of new antidiabetic agents remains the cornerstone for controlling this challenging disease in which heterocyclic compounds contributed greatly. Thiazolidinedione and quinoline nuclei exhibit different pharmacological potentials, the co...

The title compounds were prepared by brominating 1-acetylnaphthalene in chloroform followed by condensation with substituted benzaldehyde thiosemicarbazones using ethanol to get 4-naphthalen-1-yl-2-{2-[(substituted phenyl) methylidene] hydrazino}-1, 3-thiazoles. These thiazole derivatives were then cyclized to title compounds by reacting with thiom...

Targeted therapy plays a pivotal role in cancer therapeutics by countering the drawbacks of conventional treatment like adverse events and drug resistance. Over the last decade, heterocyclic derivatives have received considerable attention as cytotoxic agents by modulating various signaling pathways. Benzothiazole is an important heterocyclic scaff...

Benzimidazole and quinoline showed a large spectrum of activities in various pharmacological fields like anticonvulsant, antimicrobial, and antimalarial, including antiviral and anticancer also. The different pharmacologically active series gained the attention of many researchers, which resulted in different hybrid structure of benzimidazole and q...

Background Alzheimer’s disease (AD) is the most prevalent age-dependent neurodegenerative disease characterized by progressive impairment of memory and cognitive functions. Cyclic nucleotides like cAMP and cGMP are well-known to play an important role in learning and memory functions. Enhancement of cAMP and cGMP levels in the hippocampus by phosph...

Cancer is a kind of disease that has scared many people for many years. Cancer is due to the excessive growth of cells in every particular part of the body. Oxadiazole 1,3,4 is a magical organic moiety that has anticancer potential. Various works on the 1,3,4-oxadiazoles moiety showing anticancer activity have been reported. The present analysis su...

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...

A century after the outbreak of the Spanish flu, the world is suffering with another pandemic on because of the coronavirus. The virus took a toll of more than millions of lives worldwide and still continues to affect the health and socio-economic infrastructure all over the world. The study explores the epidemiology, etiology and transmission of t...

Benzofuran is a heterocyclic scaffold present in various natural products and possess mexcellent pharmacological properties including anti-tubercular activity as well. A novel series 26 compound containing 3-Chlorobenzofuran derivatives are designed,synthesized and spectroscopically characterized. In vitro screening of compounds was done against mu...

The research presented aims at developing Ropinirole hydrochloride (RHCl) nanoemulsion (NE) with nigella oil for Parkinson's disease (PD). In silico study was done to explore interactions of ropinirole and thymoquinone at receptor site (TNF-α and NFK-β). Ropinirole and Thymoquinone forms a hydrogen bond with residue Arginine 201 and residue Arginin...

In the present scenario, there has been a lot of consideration toward the field of free radical chemistry. Free radicals responsive oxygen species are produced by different endogenous frameworks, exposure to various physicochemical conditions, radiation, toxins, metabolized drug by-product, and pathological states. On the off chance that free radic...

Postmenopausal women are at high risk of developing breast cancer due to estrogen production in peripheral tissues of the body other than ovaries. Aromatase is present in breast tissue, leading to local estrogen production which can be inhibited by a variety of steroidal and nonsteroidal aromatase inhibitors. There are many aromatase inhibitors ava...

Introduction: A novel anticancer therapy is the need of the hour due to growing incidences of resistance to first line cancer chemotherapy. Synthetic lethality (SL) is one of the new age treatment methods being explored for combating the resistance to anticancer agents. In this method, cell mutations are exploited for the development of new therape...

Background: Vinclozolin (VCZ) is a widely used antifungal agent with capability to enter into the human food chain. VCZ metabolizes into seven metabolites M1 to M7. Several studies have shown its effects on reprotoxicity. However, there is limited information available on the interaction of VCZ metabolites with nuclear receptors. In silico studies...

Pyridazinone analogues have been known to be potential candidates for anticonvulsant agents. We have identified several pyridazinone-based anticonvulsant agents. As a continuation to our previous research, a series of hybrid pyridazinone-thiazole connected through amide linkage were designed and synthesized. Among these, compound SP-5F demonstrated...

A set of two series of 1,3,4-oxadiazole (11a-n) and 1,2,4-Triazole (12a, c, e, g, h, j-n) based topsentin analogues were prepared by replacing imizadole moiety of topsentin through a multistep synthesis starting from indole. All the compounds synthesized were submitted for single dose (10 µM) screening against a NCI panel of 60-human cancer cell li...

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...

Gliflozins constitute an important class of compounds useful as sodium glucose co-transporter (SGLT2) inhibitors to treat type-II diabetes. They act by blocking sodium-glucose transport protein 2 which is responsible for re-absorption of glucose in the proximal convoluted tubule (PCT) of kidney and thus its inhibition reduces blood glucose level. T...

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...

Introduction: About twenty patents have been published from 2013 to 2018 for developing advanced cancer therapeutics by targeting tubulin polymerization. Currently there are several tubulin inhibitors that are in the drug development pipeline for various cancers alone or in combination including antibody conjugated drugs (ACDs). Areas covered: Impo...

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

Free radicals generated due to exposure of radiation, environmental pollutants and as by-products of metabolised drugs. These free radicals are antagonized by molecules which are antioxidant in nature. Antioxidants are the substances which inhibit oxidation. They are moreover acknowledged as "free radical scavengers" as they form minor reactive spe...

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...

A series of N-substituted-3-(napthalen-2-yl)-5-substituted phenyl-4,5-dihydropyrazole-1-carbothioamide derivatives (4a-n) were synthesized with the view of structural requirements of pharmacophore for potential anticonvulsant agents. The synthesized compounds were assayed intraperitoneally (i.p.) and subcutaneously (s.c.) in mice against seizures i...

Microtubules are a protein which is made of α- and β-heterodimer. It is one of the main components of the cell which play a vital role in cell division especially in G2/M-phase. It exists in equilibrium dynamic of polymerization and depolymerization of α- and β-heterodimer. It is one of the best targets for developing anti-cancer drugs. Various nat...

Heterocyclic compounds are well known for their different biological activity. The heterocyclic analogs are the building blocks for synthesis of the pharmaceutical active compounds in the organic chemistry. These derivatives show various type of biological activity like anticancer, antiinflammatory, anti-microbial, anti-convulsant, anti-malarial, a...

To evaluate the role of COX-2 and 5-LOX as dual inhibitors in controlling the cancer cell proliferation, a set of two series having 42 compounds of 1, 2, 3-Tethered Indole-3-glyoxamide derivatives were synthesized by employing click chemistry approach and were also evaluated for their in vitro cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2), 5-l...

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...

Amyloid beta (Aβ) peptide aggregation and cholinergic neurodegeneration are involved in the development of cognitive impairment. Therefore, in this article, we examined rosuvastatin (RSV), an oral hypolipidemic drug, to determine its potential as a dual inhibitor of acetylcholinesterase (AChE) and Aβ peptide aggregation for the treatment of cogniti...

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...

Design of therapeutically viable antimicrobial peptides with cell selectivity against microorganisms is an important step towards the development of new antimicrobial agents. Here, we report four de novo designed, short amphipathic sequences based on a α-helical template comprising of Lys, Trp and Leu or their corresponding D-and/or β-amino acids....

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...

The new era of heterocyclic moieties which are developed in the decades plays a very important role in the treatment of various diseases. Amongst them are 1,3,4-oxadiazoles, a heterocyclic five member ring which plays an vital role in the development of newer medicinal compounds for treating various biological activities like proliferation of cells...

A series of new pyrimidine–triazine hybrids (4a–t) was designed and synthesized, from which potent anticonvulsant agents were identified. Most of the compounds exhibited promising anticonvulsant activity against the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) tests, along with minimal motor impairment with higher safety c...

Cytotoxicity and genotoxicity of anticancer drugs to the normal cells are major problems in cancer therapy and endanger the risk of inducing secondary malignancy. Current regimen with anticancer drugs produces various toxicities. Therefore, there is urgent need for the development of newer and safer drugs. Quinazoline derivatives occupy a pivotal p...

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...

In this paper, we report the synthesis of 2-[(6-substituted benzo[d]thiazol-2-ylcarbamoyl)methyl]-1-(4-substituted phenyl)isothiourea derivatives (4a-y) carrying active pharmacophores essential for anticonvulsant activity. The anticonvulsant activity was evaluated in vivo by maximal electroshock (MES) test and subcutaneous pentylenetetrazole (scPTZ...

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...