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2 results on '"Stammers DK"'

1. Allosteric Inhibitors against HIV-1 Reverse Transcriptase: Design and Synthesis of MKC-442 Analogues Having an Ω-Functionalized Acyclic Structure

Author

Tanaka, H, Walker, RT, Hopkins, AL, Ren, J, Jones, EY, Fujimoto, K, Hayashi, M, Miyasaka, T, Baba, M, Stammers, DK, and Stuart, DI

Abstract

Based on X-ray crystallographic analysis of MKC-442/human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) complex, analogues in which the N1-substituent is replaced with ω-functionalized alkyl groups were designed to improve the affinity for the enzyme. Synthesis of these compounds was carried out starting from MKC-442 by a sequence of reactions (N3-protection, removal of N1-ethoxymethyl group, alkylation, and N3-deprotection). The compounds were evaluated for anti-HIV activity. Structure–activity relationships are discussed in terms of the possible interaction with the enzyme.

Published
1998
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2. Closing in on HIV drug resistance.

Author

Larder BA and Stammers DK

Subjects
Catalysis, Dimerization, HIV Reverse Transcriptase chemistry, HIV Reverse Transcriptase genetics, HIV-1 enzymology, Mutation, Protein Conformation, Anti-HIV Agents pharmacology, Drug Resistance, Microbial, HIV Reverse Transcriptase metabolism, HIV-1 drug effects, Reverse Transcriptase Inhibitors pharmacology
Published
1999
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