Article
Design, synthesis and biological evaluation of a series of thioamides as non-nucleoside reverse transcriptase inhibitors.
Medicinal chemistry (Shariqah (United Arab Emirates)) - 1 Nov 2007
Mehanna Ahmed S, Belani Jitendra D, Kelley Charles J, Pallansc Luke A
Abstract excerpt
A series of thioamides were designed as bio-isosteres to the non-nucleoside reverse transcriptase inhibitor trovirdine by replacement of the thiourea NH groups with methylene groups. Eight thioamides were synthesized and in vitro tested for inhibitory effects on the activity of HIV-1 reverse transcriptase wild and mutant types. Three of the 8-thioamides exhibited enzyme inhibitory activities with IC(50) values...
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