SYNTHESIS, ANTI-VIRAL AND CYTOTOXICITY STUDIES OF SOME NOVEL N-SUBSTITUTED BENZIMIDAZOLE DERIVATIVESAbstract
A series of novel N-substituted benzimidazole derivatives were synthesized and screened anti-viral activity against a HIV -1 and -2 in MT-4 cells. New compounds were synthesized through modifying the N-1 hydrogen of benzimidazole moiety with the substitution of sulphanilamide, sulphadimidine, sulphamethoxazole, 2-aminopyridine, pthalamide, benzamide, nicotinamide, anthranilic acid and 2- marcapto- benzimidazole by mannich reaction. The structure of the synthetic compounds was characterized by means of IR and PMR data. The anti-HIV activities of the new compounds were also screened for in vitro anti-viral activity against replication of HIV-1 (IIIB) and HIV-2 (ROD) in MT-4 cells using AZT- as standard and cytostatic activity were also studied by MT- 4/MTT assay. Benzimidazole derivative BSD inhibited the replication of HIV-1 and 2 (EC50= 35.40µg/ml and CC50>125µg/ml) in MT-4 cells.
Periyasamy Selvam*, Dhani Ram Lakra and Christophe Pannecouque
Arulmigu Kalasalingam College of Pharmacy, Krishnankoil, India
14 May, 2010
13 July, 2010
12 August, 2010
01 September, 2010