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Issue 11, 2011
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Discovery of GS-8374, a potent human immunodeficiency virus type 1 protease inhibitor with a superior resistance profile

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Abstract

Introduction of a unique phosphonate moiety at the P1 position of the TMC-126 (3) scaffold provided a series of novel HIV-1 protease inhibitors (PIs) with an improved resistance profile against highly resistant variants. Optimization of the linker and phosphonate moieties lead to the identification of GS-8374 (1). Compound 1 is a potent and orally bioavailable HIV-1 PI with a superior resistance profile. Synthesis and characterization of 1 are reported.

Graphical abstract: Discovery of GS-8374, a potent human immunodeficiency virus type 1 protease inhibitor with a superior resistance profile

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Publication details

The article was received on 11 Jun 2011, accepted on 19 Jul 2011 and first published on 07 Sep 2011


Article type: Concise Article
DOI: 10.1039/C1MD00147G
Med. Chem. Commun., 2011,2, 1093-1098

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    Discovery of GS-8374, a potent human immunodeficiency virus type 1 protease inhibitor with a superior resistance profile

    G. He, Z. Yang, M. Williams, C. Callebaut, T. Cihlar, B. P. Murray, C. Yang, M. L. Mitchell, H. Liu, J. Wang, M. Arimilli, E. Eisenberg, K. M. Stray, L. K. Tsai, M. Hatada, X. Chen, J. M. Chen, Y. Wang, M. S. Lee, R. G. Strickley, Q. Iwata, X. Zheng, C. U. Kim, S. Swaminathan, M. C. Desai, W. A. Lee and L. Xu, Med. Chem. Commun., 2011, 2, 1093
    DOI: 10.1039/C1MD00147G

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