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Issue 1, 2010
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Synthesis and biological activity of new pyridone diaryl ether non-nucleoside inhibitors of HIV-1 reverse transcriptase

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Abstract

New pyridone non-nucleoside reverse transcriptase inhibitors (NNRTIs) were prepared and several flexible routes to this class of inhibitor were identified. These NNRTIs were active inhibitors of the replication of wild-type and NNRTI-resistant HIV. Structure-based drug design was used to optimize the activity of the compounds against NNRTI-resistant mutants. The co-crystal structure of inhibitor 2b in the NNRTI binding pocket of HIV reverse transcriptase (HIVRT) is also described.

Graphical abstract: Synthesis and biological activity of new pyridone diaryl ether non-nucleoside inhibitors of HIV-1 reverse transcriptase

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Publication details

The article was received on 01 Feb 2010, accepted on 01 Mar 2010 and first published on 28 Apr 2010


Article type: Concise Article
DOI: 10.1039/C0MD00009D
Citation: Med. Chem. Commun., 2010,1, 79-83

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    Synthesis and biological activity of new pyridone diaryl ether non-nucleoside inhibitors of HIV-1 reverse transcriptase

    J. J. Kennedy-Smith, N. Arora, J. R. Billedeau, J. Fretland, J. Q. Hang, G. M. Heilek, S. F. Harris, D. Hirschfeld, H. Javanbakht, Y. Li, W. Liang, R. Roetz, M. Smith, G. Su, J. M. Suh, A. G. Villaseñor, J. Wu, D. Yasuda, K. Klumpp and Z. K. Sweeney, Med. Chem. Commun., 2010, 1, 79
    DOI: 10.1039/C0MD00009D

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