the complex metabolic syndrome, diabetes mellitus, is a major human health concern in the world and is estimated to affect 300 million people by the year 2025. several drugs such as sulfonylureas and biguanides are presently available to reduce hyperglycemia in diabetes mellitus. these drugs have side effects and thus searching for a new class of compounds is essential to overcome this problems...

Abstract: Thiazole or 1,3-thiazole is a distinct heterocyclic compound which incorporates sulphur and nitrogen atoms. It vital framework present in numerous pharmacologically active compounds, be it of natural origin synthetic nature. Many thiazoles having antitumor antiviral activities, originate from microbes marine organisms. A variety drugs, thiazole group, like antimicrobial sulfathiazole,...

A new series of imidazo[2,1-b]thiazole analogs containing a methyl sulfonyl COX-2 pharmacophore was synthesized and evaluated for their COX-2 inhibitory activity. According to in-vitro COX-1/COX-2 inhibition data, all compounds (6a-g) were selective inhibitors of COX-2 isoenzyme with IC50 values in the highly potent 0.08-0.16 mM range. These results indicated that both potency and selectivity o...

A new series of imidazo[2,1-b]thiazole analogs containing a methyl sulfonyl COX-2 pharmacophore was synthesized and evaluated for their COX-2 inhibitory activity. According to in-vitro COX-1/COX-2 inhibition data, all compounds (6a-g) were selective inhibitors of COX-2 isoenzyme with IC50 values in the highly potent 0.08-0.16 mM range. These results indicated that both potency and selectivity o...

ABSTRACT. The aim of present study was the uses a series α,β-unsaturated carbonyl compounds (chalcones), in synthesis pyridine, pyran, thiophene, thiazole, together with their heterocyclic synthesis. work has resulted variety 2,5-dihydropyridine, hydrazide-hydrazone, thiophene derivatives, coumarin, pyran and thiazolo[4,5-d]thiazole derivatives. antitumor activities newly synthesized products w...

The photophysical properties and excited-state intramolecular proton transfer (ESIPT) processes for 2-(2′-hydroxyphenyl)-4-chloromethylthiazole (1), 2-(2′-hydroxyphenyl)-4-phenylthiazole (2), 2-(2′-hydroxyphenyl)-4-hydroxymethyl-thiazole (3) were studied at the TD-B3PW91/6–31 + G(d, p)/IEFPCM level. structures of 1–3 fully optimized corresponding structural parameters, infrared spectra electron...

Iodine-catalyzed regioselective sulfenylation of imidazo[1,2-a]pyridines via C(sp(2))-H bond functionalization has been achieved using sulfonyl hydrazides as a thiol surrogate. A library of 3-sulfanylimidazopyridines with broad functionalities was synthesized under metal and oxidant-free practical reaction conditions. This methodology is also applicable for the regioselective sulfenylation of i...

The biosynthesis of thiamine has been believed to be accomplished with the initial formation of the pyrimidine and thiazole moieties by independent routes, followed by a final step in which pyrimidine and thiazole are jointed together to form thiamine. Recently, Nose (1-3), Brown (4-7), and Leder (8, 9) separated the enzyme system from cell-free extracts of bakers' yeast which is capable of syn...

Quinazolinones are a group of fused heterocyclic compounds which have valuable biological properties including cytotoxic, antibacterial and antifungal activities. Thiazole group-containing compounds have been also reported to have a wide range of biological activities such as antitumor, anti-inflammatory, analgesic and antibacterial effects. Due to valuable cytotoxic effects of both thiazole gr...

The synthesis, characterization, and functional in vitro assay in cardiac and smooth muscle (vascular and nonvascular) of a series of 4-imidazo[2,1-b]thiazole-1,4-dihydropyridines are reported. To define the calcium blocker nature of the imidazo[2,1-b]thiazole-1,4-DHPs and their selectivity on Cav1.2 and Cav1.3 isoforms, we performed binding studies on guinea pig atrial and ventricular membrane...