Identification of a 3-aminoimidazo[1,2-a]pyridine inhibitor of HIV-1 reverse transcriptase

被引：28

作者：

Elleder, Daniel ^{[1
]}

Baiga, Thomas J. ^{[2
,4
]}

Russell, Rebecca L. ^{[2
]}

Naughton, John A. ^{[1
]}

Hughes, Stephen H. ^{[3
]}

Noel, Joseph P. ^{[2
]}

Young, John A. T. ^{[1
]}

机构：

[1] Salk Inst Biol Studies, Nomis Ctr Immunobiol & Microbial Pathogenesis, La Jolla, CA 92037 USA

[2] Salk Inst Biol Studies, Howard Hughes Med Inst, Jack H Skirball Ctr Chem Biol & Prote, La Jolla, CA 92037 USA

[3] NCI, HIV Drug Resistance Program, Frederick, MD 21702 USA

[4] EMD Millipore Corp, Biosci Business Unit, Pacific Ctr Court 10394, San Diego, CA 92121 USA

来源：

VIROLOGY JOURNAL | 2012年 / 9卷

关键词：

HIV-1; NNRTI; Inhibitor; IMMUNODEFICIENCY-VIRUS TYPE-1; DRUG DISCOVERY; REPLICATION; INFECTION; NNRTIS;

D O I：

10.1186/1743-422X-9-305

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

Background: Despite the effectiveness of highly active antiretroviral therapy (HAART), there remains an urgent need to develop new human immunodeficiency virus type 1 (HIV-1) inhibitors with better pharmacokinetic properties that are well tolerated, and that block common drug resistant virus strains. Methods: Here we screened an in-house small molecule library for novel inhibitors of HIV-1 replication. Results: An active compound containing a 3-aminoimidazo[1,2-a]pyridine scaffold was identified and quantitatively characterized as a non-nucleoside reverse transcriptase inhibitor (NNRTI). Conclusions: The potency of this compound coupled with its inexpensive chemical synthesis and tractability for downstream SAR analysis make this inhibitor a suitable lead candidate for further development as an antiviral drug.

引用

页数：7

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