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Allosteric inhibitors against HIV-1 reverse transcriptase: design and synthesis of MKC-442 analogues having an omega-functionalized acyclic structure.

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 omega-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 acti...

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Publication status:
Published

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Institution:
University of Oxford
Division:
MSD
Department:
NDM
Sub department:
Structural Biology
Role:
Author
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Journal:
Antiviral chemistry and chemotherapy
Volume:
9
Issue:
4
Pages:
325-332
Publication date:
1998-07-01
EISSN:
2040-2066
ISSN:
0956-3202
Source identifiers:
7799
Language:
English
Keywords:
Pubs id:
pubs:7799
UUID:
uuid:2bdd56a1-fad1-4590-9506-07ea9f192217
Local pid:
pubs:7799
Deposit date:
2012-12-19

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