Synthesis and anti-HIV activity of some novel 5-[ß-(10-phenothiazinyl)ethyl]-1-(acyl)-1,2,3,4-Tetrazoles

Abstract

Several 5-[ß-(10-phenothiazinyl)ethyl]-1-(acyl)-1,2,3,4-Tetrazoles have been synthesized and six of them were tested at the National Cancer Institute, Bethesada, Maryland, USA for their anti-HIV activity in susceptible human host cells (CEM Cell lines) over a wide range of concentrations from 6.36 x 10-8 to 2.00 x 10-4 M. (The highest protection observed is 112.84%). The most potent compound proved to be 5-[ß-(10-phenothiazinyl)ethyl]-1-(p-chlorobenzyl)-,2,3,4-Tetrazole (6) which displayed an EC50 of 3.45 x 10-6 M for inhibition of cytoprotective effect of HIV-1 in CEM cells. It exhibited cytotoxicity with an IC50 value of 6.25 x 10-5 M. The structure of these compounds has been established on the basis of elemental analysis and IR, 1H-NMR and Mass spectral data.

Keywords: HIV-1; Tetrazoles; Phenothaizines; CEM Cells

Journal of Pharmacy and Bioresources Vol. 4 (2) 2007: pp. 64-69