Studies of non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: Synthesis and structure-activity relationships of 2-cyano and 2-hydroxy thiazolidenebenzenesulfonamide derivatives

A series of thiazolidenebenzenesulfonamides was prepared and evaluated for their inhibitory effects on the WT, Y181C, and K103N reverse transcriptase (RT) activity and HIV-1 replication. The cyano derivatives 10l and 18b (YM-228855) showed extremely potent anti-HIV-1 activity. Compound 11g (YM-215389) showed the most potent activity against the WT and the two mutant RTs. Furthermore, this compound was also a highly potent inhibitor of HIV-1 replication.