A series of twelve new 2-(methylthio)-1H-benzimidazole-5-carboxamide derivatives (1−12) were synthesized and their antiparasitic activity was tested in vitro against Giardia intestinalis, Trichomonas vaginalis and Entamoeba histolytica. Experimental evaluations showed IC50 values within the nano...

Urease is an important enzyme which breaks urea into ammonia and carbon dioxide during metabolic processes. However, an elevated activity of urease causes various complications of clinical importance. The inhibition of urease activity with small molecules as inhibitors is an effective strategy f...

Thirty six new N-(4-substituted phenyl)-2-[4-(substituted) benzylidene]-hydrazinecarbothioamides were synthesized and evaluated for anticonvulsant activity and neurotoxicity. The anticonvulsant activity was established in three seizure models i.e. MES, scMET and 6 Hz model. The most active compo...

New N-(substituted)-2-[4-(substituted)benzylidene]hydrazinecarbothioamides were designed, synthesized and evaluated for anticonvulsant activity and neurotoxicity. The anticonvulsant activity was established in three seizure models i.e. MES, scMET and 6 Hz model. The most active compound was N-(4...

Development of novel, safe and effective drug candidates combating the emerging drug resistance has remained a major focus in the mainstream of anti-tuberculosis research. Here, we inspired to design and synthesize series of new pyridin-4-yl-1,3,4-oxadiazol-2-yl-thio-ethylidene-hydrazinecarbothi...

A series of N-aryl-2-phenyl-hydrazinecarbothioamides have been investigated as possible inhibitors of tyrosinase, an enzyme involved in the development of melanomas. The hydrazinecarbothioamides 1–6 were synthesized from the reaction between phenylhydrazine and isothiocyanates, for which three ...

Studies in Southern Africa have shown that whites have significantly greater morbidity and mortality from coronary heart disease than blacks. This study investigated the distribution of some haemostatic variables known or suspected to be correlated with greater risk for coronary heart disease in...

In the human antithrombin III (AT III) gene of Caucasian, two restriction fragment length polymorohism(RFLPs) have been identified and used for the linkage analysis of many congenital AT III abnormality and deficiency. In the present study, we attempted to examine the existence and distribution ...

A molecular antithrombin III variant (Antithrombin III Roma) with an abnormal pattern of crossed immunoelectrofocusing was further investigated in order to identify the pathological isoforms. AT III crossed immunoelectrofocusing of the whole plasma from the affected patients showed a loop overla...

Antithrombin III is a plasma gylcoprotein responsible for thrombin inhibition in the blood coagulation cascade. The X-ray structure of its cleaved form has been determined and refined to 3.2 Å resolution. The overall topology is similar to that of ω1-antitrypsin, another member of the serpin (s...

Cross-sectional studies suggest that both low and high antithrombin III levels are associated with the risk of arterial disease, principally ischaemic heart disease (IHD). The prospective relation between antithrombin III and subsequent death from arterial disease has been investigated in 893 me...

Tankyrases-1 and -2 (TNKS-1 and TNKS-2) have three cellular roles which make them important targets in cancer. Using NAD+ as a substrate, they poly(ADP-ribosyl)ate TRF1 (regulating lengths of telomeres), NuMA (facilitating mitosis) and axin (in wnt/β-catenin signalling). Using molecular modelli...

(2S,4S)-4-Fluoro-1-({[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino}acetyl)pyrrolidine-2-carbonitrile monofumarate (ASP8497) is a novel dipeptidyl peptidase (DPP)-IV inhibitor. In this study, we investigated the antidiabetic potency, mechanism, and duration of action of ASP8497 both in vitro a...

A series of novel N-benzylcarboxamide derivatives of bicyclic compounds, 3,4-dihydropyrido[3,2-f][1,4]oxazepin-5(2H)-one and 2,3,4,5-tetrahydro-6H-pyrido[2,3-b][1,5]oxazocin-6-one, were synthesized by cyclization of N-benzyl-2-chloro-N-(2-hydroxyethyl)- [and -(3-hydroxypropyl)-] nicotinamides, r...

The synthesis and anticancer activity of 2-arylamino-6-trifluoromethyl-3-(hydrazonocarbonyl)pyridines is described. The new trifluoromethylpyridine derivatives were evaluated for their anticancer activity toward human cancer cell lines by the National Cancer Institute (NCI). Most of them had exc...

Asymmetric conjugate addition of ethyl 4,4,4-trifluoroacetoacetate and other trifluoromethyl substituted nucleophiles to β,γ-unsaturated α-keto esters has been developed. The reaction efficiently provided dihydropyrans via cascade Michael–hemiketalization pathways. Quinine-derived thiourea w...

A facile synthesis of 3-hydroxy-3-(trifluoromethyl)-1H-pyrrol-2(3H)-ones based on trifluoroacetic acid-catalyzed condensation–cyclization reactions of β-enamino esters and ethyl trifluoropyruvate is described. These reactions afford a series of α-trifluoromethylated γ-lactam compounds in goo...

α,β-Unsaturated hydroxamates derived from the ‘chiral Weinreb amide’ auxiliary (S)-N-1-(1′-naphthyl)ethyl-O-tert-butylhydroxylamine consistently adopt a defined conformation and undergo highly diastereoselective conjugate addition reactions with lithium amide reagents. The configuration of ...

Thirteen optically active (αS, βR) 1-naphthyl keto-oxiranes (1-naphthyl-4-yl[3-(substituted phenyl)oxiran-2-yl]methanones) have been synthesised by phase transfer catalysed epoxidation of 1-naphthyl chalcones. The yields of oxiranes are more than 95%. The synthesized oxiranes have been charact...

DPP-IV inhibitors have been immersed as promising pathway to treat Type 2 diabetes. Here we have reported designing of coumarin derivatives as DPP-IV inhibitors. Designed compounds have been studied for their binding with DPP-IV enzyme through molecular docking followed by synthesis. All synthes...