All current anti-viral therapies fail to completely eradicate the human immunodeficiency type 1 (HIV-1) virus from those infected and the infection caused by HIV-1 remains incurable. Host cell restriction factors, including APOBEC3G (A3G), suppress viral replication and have emerged as a novel target for development of therapeutic and preventive agents against HIV-1 infection. A3G has been shown to block HIV-1 replication, but is degraded in HIV infected cells by the essential HIV-1 protein, virion infectivity factor (Vif). Small molecules that target the interface of Vif and A3G, thereby protecting A3G from Vif-mediated degradation, are of significant interest as potential anti-HIV therapeutics. With an ultimate aim to develop new anti-viral drugs that inhibit the A3G-Vif interaction, a series of bisaryl benzamides were designed and synthesized. Several compounds from this series were found to be effective in raising cellular levels of the A3G protein in a non-toxic manner. Their synthesis and preliminary biological evaluation will be described. Potent compounds from this series could serve as valuable tools in order to better understand the role of A3G-Vif interaction in HIV-1 and for possible clinical applications.

Substituted bisaryl benzamide derivatives to inhibit HIV-1 replication

251st National Meeting (2016)

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