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.
Substituted 1,2,4-Triazolo[3,4-b]-1,3,4-thiadiazoles. -Some of the title compounds (VI) (24 examples) show moderate antimicrobial activity against various bacterial and fungal strains. None of them, however, exhibit significant antiinflammatory and analgesic activities. -(MATHEW, V.; KESHAVAYYA*, J.; VAIDYA, V. P.; Eur.
4-Amino-5-aryl/heteroaryl substituted-3-mercapto-1,2,4-triazoles 3(a-d) were prepared from the corresponding aromatic carboxylic acids through a multi-step sequence. Compounds 3(a-d) were made to react with various aromatic/hetero aromatic acids and hetero aromatic aldehydes to give 3,6-disubstituted-1,2,4-triazolo [3,4-b]-1,3,4-thiadizoles and 3,6-disubstituted-5,6-dihydro-1,2,4-triazolo [3,4-b]-1,3,4-thiadizoles respectively. Elemental analysis, IR,1H NMR and mass spectral data elucidated the structures of all newly synthesized compounds. Synthesized compounds are studied for their antibacterial, antifungal, anti-inflammatory and analgesic activities. Some of the tested compounds showed significant pharmacological activities.
Thiadiazole derivatives R 0300 Synthesis and Pharmacological Activities of 1,2,4-Triazolo[3,4-b]1,3,4-thiadiazoles and Their Dihydro Analogues. -Some of the synthesized compounds exhibit promising antimicrobial activities as well as moderate to good anti-inflammatory and analgesic activity. -(MATHEW*, V.; GILES, D.; KESHAVAYYA, J.; VAIDYA, V. P.; Arch. Pharm. (Weinheim, Ger.) 342 (2009) 4, 210-222; Pharm. Chem., Acharya & B. M. Reddy Coll. Pharm.,
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