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Abstract

AntiHIV, antibacterial and antifungal activities of some novel 1,4-disubstituted-1,2,4-triazolo[4,3-a] quinazolin-5(4 h)-ones

Author(s): V Alagarsamy1, R Giridhar2, MR Yadav2, R Revathi1, K Ruckmani1, E De Clercq3
1 Medicinal Chemistry, R & D Laboratory, Periyar College of Pharmaceutical Sciences for Girls, Trichy-620 021, India 2 Pharmacy Department, Faculty of Technology and Engineering, The M. S. University of Baroda, Vadodara-390 001, India 3 Rega Institute for Medical Research, Minderbroederstrart-10, Belgium, India

Correspondence Address:
V Alagarsamy Medicinal Chemistry, R & D Laboratory, Periyar College of Pharmaceutical Sciences for Girls, Trichy-620 021 India E-mail: [email protected]


The title compounds 1-substituted-4-phenyl-1,2,4-triazolo[4,3-a]quinazolin-5(4 H )-ones were synthesized by the cyclization of 2-hydrazino-3-phenylquinazolin-4(3 H )-one with various one carbon donors. The starting material 2-hydrazino-3-phenylquinazolin-4(3 H )-one was synthesized from aniline. Investigation of antimicrobial activity of the test compounds was made by agar cup-plate method against 8 pathogenic bacteria including Mycobacterium tuberculosis , 3 pathogenic fungi and antiHIV activity against replication of HIV-1(IIIB) and HIV-2(ROD) in MT-4 cells. The compound 7e inhibited 21% growth of M. tuberculosis at 6.25 µg/ml concentration, while the compounds 7c and 7d showed good antifungal activity against Candida albicans ; and the compounds 7c exhibited good antifungal activity against Aspergillus niger .

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