Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs)

被引：14

作者：

Venkatraj, Muthusamy ^{[1
]}

Arien, Kevin K. ^{[2
]}

Heeres, Jan ^{[1
]}

Dirie, Bertrand ^{[1
]}

Joossens, Jurgen ^{[1
]}

Van Goethem, Sebastiaan ^{[1
]}

Van der Veken, Pieter ^{[1
]}

Michiels, Johan ^{[2
]}

Velde, Christophe M. L. Vande ^{[3
]}

Vanham, Guido ^{[2
,4
,5
]}

Lewi, Paw J. ^{[1
]}

Augustyns, Koen ^{[1
]}

机构：

[1] Univ Antwerp, Med Chem Lab, B-2610 Antwerp, Belgium

[2] Inst Trop Med, Virol Unit, Div Microbiol, Dept Biomed Sci, B-2000 Antwerp, Belgium

[3] Karel de Grote Univ Coll, Dept Appl Engn, Xray Crystallog Lab, B-2660 Antwerp, Belgium

[4] Univ Antwerp, Dept Biomed Sci, B-2610 Antwerp, Belgium

[5] Free Univ Brussels, Fac Med & Pharm, B-1090 Brussels, Belgium

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2011年 / 19卷 / 20期

关键词：

HIV-1 reverse transcriptase; NNRTIs; Diarylpyridinones; Diarylpyridazinones; Diarylphthalazinones; IMMUNODEFICIENCY-VIRUS TYPE-1; RESISTANT MUTANT VIRUSES; DIARYLPYRIMIDINE ANALOGS; ANTIVIRAL ACTIVITY; HIGHLY POTENT; BROAD POTENCY; DAPY ANALOGS; N-AMINATION; WILD-TYPE; DERIVATIVES;

D O I：

10.1016/j.bmc.2011.08.060

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

In this Letter, we report on diarylpyridinone, diarylpyridazinone and diarylphthalazinone analogs as potential inhibitors of HIV-1 nonnucleoside reverse transcriptase (NNRTIs). The most promising compounds in these series are three diarylpyridazinones 25a, 25I and 25n which demonstrated submicromolar activity against wild-type HIV-1 and moderate activity against the single mutant strain Ba-L V106A. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：5924 / 5934

页数：11

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