2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.

doi:10.1021/jm900044w

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Article

2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.

Journal of medicinal chemistry - 23 Apr 2009

Degoey David A, Grampovnik David J, Flentge Charles A, Flosi William J, Chen Hui-Ju, Yeung Clinton M, Randolph John T, Klein Larry L, Dekhtyar Tatyana, Colletti Lynn, Marsh Kennan C, Stoll Vincent, Mamo Mulugeta, Morfitt David C, Nguyen Bach, Schmidt James M, Swanson Sue J, Mo Hongmei, Kati Warren M, Molla Akhteruzzaman, Kempf Dale J

Abstract excerpt

A series of symmetry-based HIV protease inhibitors was designed and synthesized. Modification of the core regiochemistry and stereochemistry significantly affected the potency, metabolic stability, and oral bioavailability of the inhibitors, as did the variation of a pendent arylmethyl P3 group. Optimization led to the selection of two compounds, 10c (A-790742) and 9d (A-792611), for advancement to preclinical...

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PMID: 19323562
DOI: 10.1021/jm900044w

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