Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

Back

Synthesis and Anti-HIV-1 Activity of a Novel Series of Aminoimidazole Analogs

Author(s): Swastika Ganguly, Sankaran Murugesan, Naru Prasanthi, Onur Alpturk, Brian Herman, Nicolas Sluis-Cremer.

Abstract:

There is still an urgent need to develop nonnucleoside reverse transcriptase (RT) inhibitors (NNRTI) with a high-genetic barrier to resistance that facilitate patient adherence and allow durable suppression of HIV-1 replication. In this study, we describe the synthesis of a novel series of N-aminoimidazole (NAIM) analogs. Each of the NAIM analogs display potent activity against wild-type recombinant purified HIV-1 RT as well as RTs containing the K103N or Y181C resistance mutations. The analogs, however, do not exhibit significant antiviral activity in cell culture and were, in general, cytotoxic. Nevertheless, these data suggest that the NAIM backbone may provide a suitable scaffold from which inhibitors active against NNRTI-resistant HIV-1 could be developed.

Keywords: N-aminoimidazole, NNRTI, HIV, Reverse transcriptase, Synthesis, Molecular modeling

Order Reprints Order Eprints Rights & PermissionsPrintExport

Article Details

VOLUME: 7
ISSUE: 5
Year: 2010
Page: [318 - 323]
Pages: 6
DOI: 10.2174/157018010791163424
Price: $58