New 2-substituted-4-(5-phenyl-1H-tetrazol-1-yl)-2,3,5a,9a-tetrahydro-1H-1,5-benzodiazepine derivatives were synthesized by conventional as well as microwave method. Benzonitrile and sodium azide in the presence of ammonium chloride and DMF produces 5-phenyltetrazole; this on reaction with acetic anhydride forms 5-phenyl-1-acetyl tetrazole which reacted with different aromatic aldehydes in the presence of the alkaline medium, to yield corresponding chalcones. Chalcones on further reaction with o-phenylenediamine yield 2-substituted-4-(5- phenyl-1H-tetrazol-1-yl)-2,3,5a,9a-tetrahydro-1H-1,5-benzodiazepines (4a-4j). The structures of newly synthesized compounds were characterized by physical and spectral characteristics by FT-IR and 1H NMR spectroscopy. All synthesized compounds were evaluated for their antifungal activity by MIC (minimal inhibitory concentration, broth dilution method) against A. niger and C. albicans. All synthesized compounds show moderate to good antifungal activity.
Key words: chalcones; tetrazoles; antifungal activity; 2-substituted 4-(5-phenyl-1H-tetrazol-1-yl)-2,3,5a,9a-tetrahydro-1H-1,5- benzodiazepines
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