Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase

Juliana Ruiz-Caro; Aravind Basavapathruni; Joseph T. Kim; Christopher M. Bailey; Ligong Wang; Karen S. Anderson; Andrew D. Hamilton; William L. Jorgensen

doi:10.1016/j.bmcl.2005.10.037

Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase

Juliana Ruiz-Caro, Aravind Basavapathruni, Joseph T. Kim, Christopher M. Bailey, Ligong Wang, Karen S. Anderson, Andrew D. Hamilton, William L. Jorgensen

Chemistry

Research output: Contribution to journal › Article › peer-review

Abstract

Following computational analyses, potential non-nucleoside inhibitors of HIV-1 reverse transcriptase have been pursued through synthesis and assaying for anti-viral activity. The general class Het-NH-Ph-U has been considered, where Het is an aromatic heterocycle and U is an unsaturated, hydrophobic group. Results for compounds with Het = 2-thiazoyl and 2-pyrimidinyl are the focus of this report.

Original language	English (US)
Pages (from-to)	668-671
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	3
DOIs	https://doi.org/10.1016/j.bmcl.2005.10.037
State	Published - Feb 1 2006

Keywords

Anti-HIV drug
Computer-aided drug design
Diarylamine
NNRTI
Pyrimidinylamine
Thiazoylamine

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2005.10.037

Cite this

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title = "Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase",

abstract = "Following computational analyses, potential non-nucleoside inhibitors of HIV-1 reverse transcriptase have been pursued through synthesis and assaying for anti-viral activity. The general class Het-NH-Ph-U has been considered, where Het is an aromatic heterocycle and U is an unsaturated, hydrophobic group. Results for compounds with Het = 2-thiazoyl and 2-pyrimidinyl are the focus of this report.",

keywords = "Anti-HIV drug, Computer-aided drug design, Diarylamine, NNRTI, Pyrimidinylamine, Thiazoylamine",

author = "Juliana Ruiz-Caro and Aravind Basavapathruni and Kim, {Joseph T.} and Bailey, {Christopher M.} and Ligong Wang and Anderson, {Karen S.} and Hamilton, {Andrew D.} and Jorgensen, {William L.}",

note = "Funding Information: Gratitude is expressed to the National Institutes of Health (AI44616, GM35208, and GM49551) for support. ",

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AU - Ruiz-Caro, Juliana

AU - Basavapathruni, Aravind

AU - Kim, Joseph T.

AU - Bailey, Christopher M.

AU - Wang, Ligong

AU - Anderson, Karen S.

AU - Hamilton, Andrew D.

AU - Jorgensen, William L.

N1 - Funding Information: Gratitude is expressed to the National Institutes of Health (AI44616, GM35208, and GM49551) for support.

PY - 2006/2/1

Y1 - 2006/2/1

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AB - Following computational analyses, potential non-nucleoside inhibitors of HIV-1 reverse transcriptase have been pursued through synthesis and assaying for anti-viral activity. The general class Het-NH-Ph-U has been considered, where Het is an aromatic heterocycle and U is an unsaturated, hydrophobic group. Results for compounds with Het = 2-thiazoyl and 2-pyrimidinyl are the focus of this report.

KW - Anti-HIV drug

KW - Computer-aided drug design

KW - Diarylamine

KW - NNRTI

KW - Pyrimidinylamine

KW - Thiazoylamine

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Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase

Abstract

Keywords

ASJC Scopus subject areas

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