Z. Brzozowski, F. Sa̧czewski
2007
Citations
0
Influential Citations
7
Citations
Quality indicators
Journal
Journal of Heterocyclic Chemistry
Abstract
A series of N-(3-amino-3,4-dihydro-4-oxopyrimidin-2-yl)-4-chloro-2-mercapto-5-methylbenzenesulfonamide derivatives 10-17 have been synthesized as potential anti-HIV agents. The in vitro anti-HIV-1 activity of these compounds has been tested at the national Cancer Institute (Bethesda, MD), and the structure-activity relationships are discussed. The selected N-[3-amino-3,4-dihydro-6-(tert-butyl)-4-oxothieno[2,3-e]pyrimidin-2-yl]-4-chloro-2-metcapto-5-methylbenzenesulfonamide (14) showed good anti-HIV-1 activity with 50% effective concentration (EC50) value of 15 μM and weak cytotoxic effect (IC50 = 106 μM).