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Thiadiazole derivatives R 0300Studies on Synthesis and Pharmacological Activities of 3,6-Disubstituted-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles and Their Dihydro Analogues. -Several triazolothiadiazoles (IV) (27 examples) and related dihydro derivatives (VI) (12 examples) are synthesized by condensation of mercaptotriazoles (II) with carboxylic acids or aldehydes, respectively. Some of the products show significant antimicrobial [e.g. (IVd)] or good antiinflammatory and analgesic activities [e.g. (IVf)]. -(MATHEW*, V.; KESHAVAYYA, J.; VAIDYA, V. P.; GILES, D.; Eur. J. Med. Chem. 42 (2007) 6, 823-840; Pharm. Chem., Acharya & B. M. Reddy Coll. Pharm., Bangalore 560 090, India; Eng.) -A. Forchert 42-124

4-Amino-5-substituted aryl-3-mercapto-1,2,4-triazoles are versatile synthons for constructing various biologically active heterocycles. Starting from 4-amino-5-substituted aryl-3-mercapto-1,2,4-triazole 3a-c, a series of new 3,5-disubstituted-1,2,4-triazolo-[3,4-b]1,3,4-thiadiazoles and their 5,6-dihydrotriazolothiadiazoles were prepared. The structures of all the newly synthesized compounds have been confirmed by elemental analysis, IR,( 1)H-NMR, (13)C-NMR, and mass spectra. The antimicrobial effects of the synthesized compounds were investigated using the paper disc method. Anti-inflammatory and analgesic activities of the synthesized compounds were assessed by carrageenan-induced rat paw oedema method and by Eddy's hot plate method, respectively. Some of the compounds exhibited promising antimicrobial activities as well as moderate to good anti-inflammatory activity and analgesic activity.

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