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

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

Volume: 7 Issue: 5

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

Affiliation:

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

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.

Cite this article as:

Ganguly Swastika, Murugesan Sankaran, Prasanthi Naru, Alpturk Onur, Herman Brian and Sluis-Cremer Nicolas, Synthesis and Anti-HIV-1 Activity of a Novel Series of Aminoimidazole Analogs, Letters in Drug Design & Discovery 2010; 7 (5) . https://dx.doi.org/10.2174/157018010791163424