Department of Chemical Technology of Drugs, Medical University of Gdańsk, Al. Gen. Hallera 107, 80‐416 Gdańsk, Poland
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‐oxothieno2,3‐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).