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Abstract

Anti HIV, Antibacterial And Antifungal Potential Of A Variety Of Heterocyclic Compounds Containing Nitrogen And/Or Sulphur

Author(s): S. M Sondhi, R. P Verma, Nidhi Singhal, V. K Sharma, C Husiu, L Vargiu, S Longu, P. LA Colla

9-Acridinyl imino/amino derivatives (Ia-f, IIa-b, III, IV and V), pyrimido oxazole derivative (VIa), imidazopyrimidine thiones (VIb, VII), pyrimidooxazinethione (VIc), 1-(2-aminoaryl)-6-hydroxy-4,4,6-trimethyl-1,4,5,6-tetrahydropyrimidine-2(3H)-thiones (VIIIa-c), 1-(2-nitroaryl)-6-methoxy-6-methyl-1,4,5,6-tetrahydro pyrimidine-2-(3H) thiones (IXa,b), 1-(2-hydroxy phenyl)-4,4,6-trimethyl-1,4-dihydropyrimidine-2(3H)-thione (X), condensed tricyclic pyrimidine derivatives (XIa-h) pyrimido anthraquinonimidazole (XII), N,N'-disubstituted thioureas (XIIIa-c), 1,2-dithia-5,8-diazacyclodeca-4,8-diene (XIV), 1,2-dithia-5,8-diazacyclodecane dihydrochloride (XV), 3-(o-aminophenyl)-2-imino-4-phenyl-4-thiazoline (XVI), 9H-Imidazolo[1,2-a] benzimidazoles (XVIIa-c), benzimidazole derivative (XVIII), Schiff's bases (XIX, XXa-b), 1-(2-methylamino-4-phenyl thiazole)-2-hydroxy-naphthalene (XXI), compound XXII and acridone derivative XXIII were synthesized by the procedures developed earlier and were screened for anti HIV, antibacterial and antifungal activities. Compounds XVIIb and XVIIc showed antibacterial activity against Streptococcus D at concentrations slightly higher than those of streptomycin (1.6 µM) and compound XV showed mild activity against Salmonella (MIC = 66 µM). When tested against yeast representatives, compound XV was active against C-neoformans (MIC = 22 µM), compounds XV and XXa showed mild activity against Candida at 66 µM but this concentration was cytotoxic for MT-4 cells. Only compound XIa was capable of protecting MT-4 cells from the cytopathic effect induced by HIV -1 (EC50 = 115 µM). All other compounds were found to be inactive.

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