HIV integrase strand transfer inhibitors (InSTIs) are an important class of antiviral agents for HIV infections. Merck’s Raltegravir, the first marketed InSTi, has demonstrated excellent efficacy and tolerability in treating HIV patients. To further improve its viral mutation and pharmacokinetic profiles, we discuss a medicinal chemistry campaign based on the 2-pyridone aminal pharmacophore <b>1</b>. With a combination of singleton and parallel medicinal chemistry approaches, the impact of modulating the R1 benzyl moiety on the overall profile of this class of compounds has been evaluated. Novel heterocyclic benzyl moieties have been identified. Herein, we discuss our findings from this effort.

Optimization of the benzyl moiety in 2-pyridone aminals as HIV integrase strand transfer inhibitors (InSTIs)

2019 Fall National Meeting

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