Free fatty acid receptor 1 (FFA1), previously known as GPR40 is a G protein-coupled receptor and a new target for treatment of type 2 diabetes. Two series of FFA1 agonists utilizing a 1,3,4-thiadiazole-2-caboxamide scaffold were synthetized. Both series offered significant improvement of the potency compared to the previously described 1,3,4-thiadiazole-based FFA1 agonists and high selectivity ...

This review article presents a survey of the utility of a new synthetic strategy for 1,3,4-thiadiazole derivatives based on reactions of nitrilimines with various functionalized sulfur dipolarophiles which proceed via tandem in situ 1,3-dipolar cycloaddition and β-elimination of simple molecule from the initially formed cycloadduct. The biological activities of some of the compounds prepared by...

in the recent years, the role of lox enzymes in the cause of neoplastic diseases such as colorectal, skin, pancreatic and renal cancers has been confirmed. a new series of 1,3,4-thiadiazole derivatives bearing 2-pyridyl moiety was synthesized and their cytotoxicity was assessed using mtt protocol. enzyme inhibitory activity of prepared compounds was also tested against 15-lipoxygenase-1 as nove...

The effect of nicotinamide and a variety of nicotinamide analogs and related corn pounds on the activity of 92-amino-1,3,4-thiadiazole against transplanted mouse leu kemia B892 has been tested. 5-Fluoronicotinamide, 6-aminonicotinamide, N-hydroxy bis-methylnicotinamide, N-N'-methylene-bis-nicotinamide, DPN, and 3-acetylpyridine were as potent as nicotinamide and nicotinic acid in reversing the ...