Research
Identification of a 3-aminoimidazo[1,2-a]pyridine inhibitor of HIV-1 reverse transcriptase
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
Virology Journal 2012, 9:305 doi:10.1186/1743-422X-9-305
Published: 11 December 2012Abstract
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.
