Discovery of an HIV integrase inhibitor with an excellent resistance profile

…, H Vuong, DC Blakemore, D Stead, C Ashcroft…

Index: Pryde, David C.; Webster, Rob; Butler, Scott L.; Murray, Edward J.; Whitby, Kevin; Pickford, Chris; Westby, Mike; Palmer, Michael J.; Bull, David J.; Vuong, Hannah; Blakemore, David C.; Stead, Darren; Ashcroft, Christopher; Gardner, Iain; Bru, Claire; Cheung, Wai-Yee; Roberts, Ieuan O.; Morton, Jennifer; Bissell, Richard A. MedChemComm, 2013 , vol. 4, # 4 p. 709 - 719

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Citation Number: 6

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 human pharmacokinetics, the results of which are ...