Discovery of an HIV integrase inhibitor with an excellent resistance profile

MedChemComm
2013.0

Abstract

In the present article, we describe SAR studies within a series of N-hydroxy-dihydronaphthyridinone HIV integrase inhibitors that led to a candidate compound, PF-4776548, of high potency and with an excellent resistance profile. Uncertainties around the human pharmacokinetic predictions for PF-4776548 led to the compound being taken into a human microdose study to confirm its humanpharmacokinetics, the results of which are described herein.

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