Synthesis and biological activity of new pyridone diaryl ether non-nucleoside inhibitors of HIV-1 reverse transcriptase

被引：21

作者：

Kennedy-Smith, Joshua J. ^{[1
]}

Arora, Nidhi ^{[1
]}

Billedeau, J. Roland ^{[1
]}

Fretland, Jennifer ^{[5
]}

Hang, Julie Q. ^{[4
]}

Heilek, Gabrielle M. ^{[3
]}

Harris, Seth F. ^{[2
]}

Hirschfeld, Donald ^{[1
]}

Javanbakht, Hassan ^{[3
]}

Li, Yu ^{[4
]}

Liang, Weiling ^{[1
]}

Roetz, Ralf ^{[1
]}

Smith, Mark ^{[1
]}

Su, Guoping ^{[3
]}

Suh, Judy M. ^{[1
]}

Villasenor, Armando G. ^{[2
]}

Wu, Jeffrey ^{[1
]}

Yasuda, Dennis ^{[1
]}

Klumpp, Klaus ^{[4
]}

Sweeney, Zachary K. ^{[1
]}

机构：

[1] Roche Palo Alto, Dept Med Chem, Palo Alto, CA 94304 USA

[2] Roche Palo Alto, Dept Discovery Technol, Palo Alto, CA 94304 USA

[3] Roche Palo Alto, Dept Viral Dis Biol, Palo Alto, CA 94304 USA

[4] Roche Palo Alto, Dept Viral Dis Biochem, Palo Alto, CA 94304 USA

[5] Roche Palo Alto, Dept Nonclin Safety, Palo Alto, CA 94304 USA

来源：

MEDCHEMCOMM | 2010年 / 1卷 / 01期

关键词：

DISCOVERY;

D O I：

10.1039/c0md00009d

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：

New pyridone non-nucleoside reverse transcriptase inhibitors (NNRTIs) were prepared and several flexible routes to this class of inhibitor were identified. These NNRTIs were active inhibitors of the replication of wild-type and NNRTI-resistant HIV. Structure-based drug design was used to optimize the activity of the compounds against NNRTI-resistant mutants. The co-crystal structure of inhibitor 2b in the NNIZTI binding pocket of HIV reverse transcriptase (HIVRT) is also described.

引用

页码：79 / 83

页数：5

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