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

MedChemComm Pub Date: 2011-09-07 DOI: 10.1039/C1MD00147G

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.

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MedChemComm

Journal Name：MedChemComm

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