Cosalane and its Analogues: A Unique Class of Anti-HIV Agents

Peng      Zhan; Zhenyu      Li; Xinyong      Liu

Abstract

Cosalane and related compounds are a peculiar group of anti-HIV agents with activities against a broad range of viral targets, such as viral entry and reverse transcriptase (RT). Cosalane and its analogues having anionic pharmacophore inhibit the binding of gp120 to CD4 as well as the fusion of the viral envelope with the cell membrane. The alkenyldiarylmethanes (ADAMs), characterized by the lack of the steroidal moiety of cosalane, are a unique class of nonnucleoside reverse transcriptase inhibitors (NNRTIs) that have potential value in the treatment of HIV infection. In this article, the structural modifications, structure-activity relationship (SAR) studies and/or crystallographic studies of cosalane related derivatives as potent antiviral agents were reviewed, which will be beneficial to the discovery of next generation cosalane derivatives with improved antiviral potency, metabolic stability and bioavailability.

Keywords: cosalane, AIDS, HIV, inhibitors, gp120, CD4, reverse transcriptase (RT), non-nucleoside RT inhibitors (NNRTIs), ADAMs