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Design of MKC-442 (emivirine) analogues with improved activity against drug-resistant HIV mutants.

Abstract:

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 close contacts with the conserved residue Trp229. Both compounds showed approximat...

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Publication status:
Published

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Publisher copy:
10.1021/jm990192c

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Journal:
Journal of medicinal chemistry More from this journal
Volume:
42
Issue:
22
Pages:
4500-4505
Publication date:
1999-11-01
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
Language:
English
Keywords:
Pubs id:
pubs:20738
UUID:
uuid:cc2230f2-61c0-4cc6-8094-dbd16ee0108e
Local pid:
pubs:20738
Source identifiers:
20738
Deposit date:
2012-12-19

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