Discovery of an HIV integrase inhibitor with an excellent resistance profile

Discovery of an HIV integrase inhibitor with an excellent resistance profile

Med. Chem. Commun., 2013, Advance Article

DOI: 10.1039/C3MD00014A, Concise Article

David C. Pryde, Rob Webster, Scott L. Butler, Edward J. Murray, Kevin Whitby, Chris Pickford, Mike Westby, Michael J. Palmer, David J. Bull, Hannah Vuong, David C. Blakemore, Darren Stead, Christopher Ashcroft, Iain Gardner, Claire Bru, Wai-Yee Cheung, Ieuan O. Roberts, Jennifer Morton, Richard A. Bissell

PFIZER GLOBAL, KENT, UK

Structure-activity relationship studies within a series of N-hydroxy-dihydronaphthyridinone HIV integrase inhibitors led to a candidate compound, of high potency and with an excellent resistance profile.

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 human pharmacokinetics, the results of which are described herein.

DOI: 10.1039/C3MD00014A

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