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...

background: cutaneous leishmaniasis (cl) is endemic in many tropical and subtropical regions of the world. due to the prolonged duration of therapy, adverse effect and resistance to current drugs in the treatment of cl, the dis­covery of novel, efficient, and safe leishmanicidal drugs is required. the aims of the present study was to synthesis of new compounds based on the active compounds of 5...

Reaction of thionyl chloride with 2-acetyl-1- benzenesulfonylpyrrole semicarbazone (6 c) gave 4 - (1- benzenesulfonyl-2 - pyrrolyl) - 1, 2, 3 -thiadiazole (lc). Selenium dioxide oxidation of 2-acetylpyrazine semicarbazone (10) in acetic acid afforded 4- (2-pyrazinyl) - 1, 2, 3- selenadiazole (4). Reaction of thionyl chloride with compound 10 gave 4- (2-pyrazinyl) - 1, 2, 3- thiadiazole (3)....

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 ...

A series of 1-(2-hydroxyethyl)-3,5-dimethylpyrazolylazo derivatives, incorporating thiosemicarbazide 2a-c, 1,3,4-thiadiazole 3a-c, and 1,2,4-triazole-3-thione 4a-c were synthesized. The structure of these novel synthesized compounds 2a-c, 3a-c, and 4a-c was confirmed by spectral analysis. All these compounds were screened for their analgesic activity. Hot-plate and tail-immersion tests were use...

1,3,4-Thiadiazole and sugar-derived molecules have proven to be promising agrochemicals with growth promoting, insecticidal and fungicidal activities. In the research field of agricultural fungicide, applying union of active group we synthesized a new set of 1,3,4-thiadiazole xylofuranose derivatives and all of the compounds were characterized by 1H NMR and HRMS. In precise toxicity measurement...