There is currently no cure for HIV-AIDS. It is known that the HIV lifecycle occurs in 10 distinct stages and according to the US Food and Drug Administration data, there are currently &gt;30 commercially prescribed drugs to treat HIV. One stage of the HIV lifecycle is integration of viral DNA into the host cell nucleus by the HIV-integrase enzyme. It has been shown that small molecule quinoline structures can effectively disrupt the integration process through an agglomeration phenomenon called multimerization. Recent x-ray crystallographic data has shown that the R1 region of the molecule plays an important role in increasing this multimerization phenomenon. The goal of this research is to investigate the chemical syntheses of quinolines substituted at the R1 region to be studied as small molecule HIV integrase inhibitors. The installation of hydrogen bond donor-acceptor functional groups at the R1 position of the quinoline pharamacophore will increase the mulitmerization of integrase enzyme effectively shutting down viral replication leading to decreased host viral reservoirs. In this presentation, we will discuss our on-going efforts to construct multi-substituted quinoline rings for structure activity relationship studies.

Investigation of quinolines as HIV-integrase inhibitors

ACS Spring Meeting 2021

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