Madurahydroxylactone Derivatives as Dual Inhibitors of Human Immunodeficiency Virus Type 1 Integrase and RNase H

A series of 29 madurahydroxylactone derivatives was evaluated for dual inhibition of human immunodeficiency virus type 1 (HIV-1) integrase and RNase H. While most of the compounds exhibited similar potencies for both enzymes, two of the derivatives showed 10- to 100-fold-higher selectivity for each...

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Main Authors: Marchand, Christophe, Beutler, John A., Wamiru, Antony, Budihas, Scott, Möllmann, Ute, Heinisch, Lothar, Mellors, John W., Le Grice, Stuart F., Pommier, Yves
Formato: Artigo
Idioma:English
Publicado em: American Society for Microbiology (ASM) 2008
Assuntos:
Antiviral Agents
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC2223906/
https://ncbi.nlm.nih.gov/pubmed/17967911
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1128/AAC.00883-07
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spelling pubmed-22239062008-04-30 Madurahydroxylactone Derivatives as Dual Inhibitors of Human Immunodeficiency Virus Type 1 Integrase and RNase H Marchand, Christophe Beutler, John A. Wamiru, Antony Budihas, Scott Möllmann, Ute Heinisch, Lothar Mellors, John W. Le Grice, Stuart F. Pommier, Yves Antimicrob Agents Chemother Antiviral Agents A series of 29 madurahydroxylactone derivatives was evaluated for dual inhibition of human immunodeficiency virus type 1 (HIV-1) integrase and RNase H. While most of the compounds exhibited similar potencies for both enzymes, two of the derivatives showed 10- to 100-fold-higher selectivity for each enzyme, suggesting that distinct pharmacophore models could be generated. This study exemplifies the common and divergent structural requirements for the inhibition of two structurally related HIV-1 enzymes and demonstrates the importance of systematically screening for both integrase and RNase H when developing novel inhibitors. American Society for Microbiology (ASM) 2008-01 2007-10-29 /pmc/articles/PMC2223906/ /pubmed/17967911 http://dx.doi.org/10.1128/AAC.00883-07 Text en Copyright © 2008, American Society for Microbiology
institution US National Library of Medicine
collection PubMed Central
language English
format Article
topic Antiviral Agents
spellingShingle Antiviral Agents
Marchand, Christophe
Beutler, John A.
Wamiru, Antony
Budihas, Scott
Möllmann, Ute
Heinisch, Lothar
Mellors, John W.
Le Grice, Stuart F.
Pommier, Yves
Madurahydroxylactone Derivatives as Dual Inhibitors of Human Immunodeficiency Virus Type 1 Integrase and RNase H
description A series of 29 madurahydroxylactone derivatives was evaluated for dual inhibition of human immunodeficiency virus type 1 (HIV-1) integrase and RNase H. While most of the compounds exhibited similar potencies for both enzymes, two of the derivatives showed 10- to 100-fold-higher selectivity for each enzyme, suggesting that distinct pharmacophore models could be generated. This study exemplifies the common and divergent structural requirements for the inhibition of two structurally related HIV-1 enzymes and demonstrates the importance of systematically screening for both integrase and RNase H when developing novel inhibitors.
author Marchand, Christophe
Beutler, John A.
Wamiru, Antony
Budihas, Scott
Möllmann, Ute
Heinisch, Lothar
Mellors, John W.
Le Grice, Stuart F.
Pommier, Yves
author_facet Marchand, Christophe
Beutler, John A.
Wamiru, Antony
Budihas, Scott
Möllmann, Ute
Heinisch, Lothar
Mellors, John W.
Le Grice, Stuart F.
Pommier, Yves
author_sort Marchand, Christophe
title Madurahydroxylactone Derivatives as Dual Inhibitors of Human Immunodeficiency Virus Type 1 Integrase and RNase H
title_short Madurahydroxylactone Derivatives as Dual Inhibitors of Human Immunodeficiency Virus Type 1 Integrase and RNase H
title_full Madurahydroxylactone Derivatives as Dual Inhibitors of Human Immunodeficiency Virus Type 1 Integrase and RNase H
title_fullStr Madurahydroxylactone Derivatives as Dual Inhibitors of Human Immunodeficiency Virus Type 1 Integrase and RNase H
title_full_unstemmed Madurahydroxylactone Derivatives as Dual Inhibitors of Human Immunodeficiency Virus Type 1 Integrase and RNase H
title_sort madurahydroxylactone derivatives as dual inhibitors of human immunodeficiency virus type 1 integrase and rnase h
publisher American Society for Microbiology (ASM)
publisher_facet American Society for Microbiology (ASM)
publishDate 2008
url https://ncbi.nlm.nih.gov/pmc/articles/PMC2223906/
https://ncbi.nlm.nih.gov/pubmed/17967911
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1128/AAC.00883-07
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