N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase

A series of N1-alkyl pyrimidinediones were designed, synthesized and evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Our efforts identified compound 10b, which represents the lead compound in this series with pharmacokinetics and antiviral potency that may support once-daily dosing.

Graphical abstractEvaluation of a series of N1-alkyl pyrimidinediones as HIV-1 non-nucleoside reverse transcriptase inhibitors identified compound 10b, which represents the lead compound with pharmacokinetics and antiviral potency that may support once-daily dosing.Figure optionsDownload full-size imageDownload as PowerPoint slide