Article
Design of MKC-442 (emivirine) analogues with improved activity against drug-resistant HIV mutants.
Journal of medicinal chemistry - 4 Nov 1999
Hopkins A L, Ren J, Tanaka H, Baba M, Okamato M, Stuart D I, Stammers D K
Abstract excerpt
Two analogues of the nonnucleoside inhibitor of HIV-1 RT, MKC-442 (emivirine), containing different C6 substituents have been designed to be less susceptible to the commonly found drug-resistance mutation of Tyr181Cys. Compound TNK-6123 had a C6 thiocyclohexyl group designed to have more flexibility in adapting to the mutated drug-binding site. GCA-186 had additional 3',5'-dimethyl substituents aimed at forming...
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