The complete eradication of human immunodeficiency virus type 1 (HIV-1) from infected individuals is complicated by HIV latency, the ability of the virus to remain quiescent within certain immune cell lines. The “shock and kill” approach has been proposed to reactivate latent proviruses and eliminate the virus in vivo. In principle this can be accomplished using a histone deacetylase (HDAC) inhibitor to reverse latency and an HIV-1 protease inhibitor to eradicate the virus. Known macrocyclic inhibitors of HIV-1 protease and HDAC2, 1 and 2, respectively, were synthesized and studied using 2D NMR techniques to establish their structures in solution. Those structures were used in computational docking experiments to design a hybrid HIV protease/HDAC inhibitor, 3. The design, synthesis and evaluation of 3 will be presented.

Design and synthesis of a dual-action agent capable of simultaneously activating HIV-1 latency and preventing new infection

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