Jump to main content
Jump to site search
Access to RSC content Close the message box

Continue to access RSC content when you are not at your institution. Follow our step-by-step guide.


Issue 4, 2013
Previous Article Next Article

Discovery of an HIV integrase inhibitor with an excellent resistance profile

Author affiliations

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

Back to tab navigation

Supplementary files

Article information


Submitted
11 Jan 2013
Accepted
11 Feb 2013
First published
15 Feb 2013

Med. Chem. Commun., 2013,4, 709-719
Article type
Concise Article

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

Search articles by author

Spotlight

Advertisements