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Open Access Research

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

Daniel Elleder14, Thomas J Baiga25, Rebecca L Russell2, John A Naughton1, Stephen H Hughes3, Joseph P Noel2 and John AT Young1*

Author Affiliations

1 The Salk Institute for Biological Studies, Nomis Center for Immunobiology and Microbial Pathogenesis, 10010 North Torrey Pines Road, La Jolla, CA 92037, USA

2 The Salk Institute for Biological Studies, Howard Hughes Medical Institute, Jack H. Skirball Center for Chemical Biology and Proteomics, 10010 North Torrey Pines Road, La Jolla, CA, 92037, USA

3 HIV Drug Resistance Program, National Cancer Institute-Frederick, Frederick, MD, 21702, USA

4 Current Address: Institute of Molecular Genetics, Academy of Sciences of the Czech Republic, Videnska 1083, Prague, Czech Republic

5 EMD Millipore Corporation, Bioscience Business Unit, 10394 Pacific Center Court, San Diego, CA, 92121, USA

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Virology Journal 2012, 9:305  doi:10.1186/1743-422X-9-305

Published: 11 December 2012

Abstract

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.

Keywords:
HIV-1; NNRTI; Inhibitor