HIV-1 integrase (IN) is a key component in virus replication and has been established as a promising multifunctional therapeutic target. Allosteric IN inhibitors (ALLINIs) have recently been classified as an effective class of antiretroviral agents. Particularly, quinoline-based ALLINIs have been shown to effectively impair HIV-1 replication, highlighting the essential nature of these heterocyclic scaffolds. In this endeavor, we have developed a synthetic strategy for the preparation of a library of quinoline scaffolds containing a meta-substituted aromatic ring at the 4-position of quinoline. This presentation will focus on the development of these quinolines as drug candidates, highlighting the synthetic route and challenges that were faced during the synthesis. Additionally, a brief comparison to other quinoline based ALLINIs will be discussed regarding the inhibition of IN.<br/>

Synthesis of tri-substituted quinolines as drug candidates for HIV-1 integrase inhibition

255th National Meeting (2018)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.