New Approaches for the Synthesis of 1,3,4-Thiadiazole and 1,2,4-Triazole Derivatives with Antimicrobial Activity

Authors: Wardakhan, Wagnat; El-Sayed, Nahed

Source: Phosphorus, Sulfur, and Silicon and the Related Elements, Volume 184, Number 3, March 2009 , pp. 790-804(15)

Publisher: Taylor and Francis Ltd

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Abstract:

The thiosemicarbazide derivatives 3a and 3b were cyclized in the presence of concentrated sulfuric acid to give the 5-cyanomethyl-1,3,4-thiadiazole derivatives 4a and 4b, respectively. The latter products were used for many heterocyclic transformations to form coumarin, 1,3,4-thiadiazolo[4,5-a]pyridine, and 5-thiophenylthiophene. In addition, compound 3b underwent cyclization in NaOH (2 N) solution to give the 1,2,4-triazole derivative 16. The reactivity of the latter product towards some chemical reagents was studied. The antimicrobial activities of the newly synthesized products were measured and showed high activities.

Keywords: Antimicrobial; coumarin; thiadiazole; triazole

Document Type: Research article

DOI: http://dx.doi.org/10.1080/10426500802274534

Affiliations: 1: National Organization for Drug Control and Research (NODCAR), Cairo, Egypt

Publication date: 2009-03-01