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Issue 4, 2013
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Discovery of an HIV integrase inhibitor with an excellent resistance profile

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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 described herein.

Graphical abstract: Discovery of an HIV integrase inhibitor with an excellent resistance profile

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Publication details

The article was received on 11 Jan 2013, accepted on 11 Feb 2013 and first published on 15 Feb 2013


Article type: Concise Article
DOI: 10.1039/C3MD00014A
Citation: Med. Chem. Commun., 2013,4, 709-719
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    Discovery of an HIV integrase inhibitor with an excellent resistance profile

    D. C. Pryde, R. Webster, S. L. Butler, E. J. Murray, K. Whitby, C. Pickford, M. Westby, M. J. Palmer, D. J. Bull, H. Vuong, D. C. Blakemore, D. Stead, C. Ashcroft, I. Gardner, C. Bru, W. Cheung, I. O. Roberts, J. Morton and R. A. Bissell, Med. Chem. Commun., 2013, 4, 709
    DOI: 10.1039/C3MD00014A

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