Journal
LETTERS IN DRUG DESIGN & DISCOVERY
Volume 9, Issue 7, Pages 687-693Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/157018012801319526
Keywords
Antibacterial activity; Antifungal activity; Minimum inhibitory concentration; Synthesis; Triazole derivatives; 1,2,4-Triazole-5(4H)-thione
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Funding
- University of KwaZulu-Natal
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A new series of 1,2,4-triazole derivatives 3a-i of (E)-4-(4-substitutedbenzylideneamino)-3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-1H-1,2,4-triazole-5(4H)-thione (2) were synthesized, deriving from 4-amino-3-((5-phenyl-1,3,4-oxadiazol-2-yl) methyl-1H-1,2,4-triazole-5(4H)-thione (1). The compounds were elucidated by IR, H-1 NMR, C-13 NMR, MS and elemental analyses. These compounds were screened for their antimicrobial activity. Among the synthesized compounds (E)-4-(4-chlorobenzylideneamino)-3-((5-phenyl-1,3,4-oxadiazol-2-yl) methyl)-2-(morpholinmethyl)-1H-1,2,4-triazole-5(4H)-thione, 3c was found to exhibit most potent In vitro antimicrobial activity with minimum inhibitory concentrations (MIC) of 1.56, 3.125, 1.56, 25, 25 and 25 mu g/ml against E. coli, S. typhimurium, L. monocytogenes, S. aureus, P. aeruginosa and S. pyogenes respectively. Compound (E)-4-(benzylideneamino)-3-((5-phenyl-1,3,4-oxadiazol-2-yl) methyl)-2-(morpholinmethyl)-1H-1,2,4-triazole-5(4H)-thione 3a was found to exhibit most potent In vitro antifungal activity with MICs 0.78 and 0.097 mu g/ml against C. albicans and F. solani.
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