Development of 2-pyrrolidinyl-N-methyl pyrimidones as potent and orally bioavailable HIV integrase inhibitors.

Marco Ferrara, Fabrizio Fiore, Vincenzo Summa, Cristina Gardelli

Department of Medicinal Chemistry IRBM-MRL, Pomezia (RM), Italy. marco.ferrara@boehringer-ingelheim.com

Bioorganic & medicinal chemistry letters 2010 Sep 1

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A series of 2-pyrrolidinyl-N-methyl pyrimidones HIV integrase inhibitors has been explored leading to the identification of derivative 13, which showed high activity at inhibiting viral replication in cell culture, favorable pharmacokinetic profile in two preclinical species, and an attractive profile against a panel of HIV-integrase mutants. Copyright 2010 Elsevier Ltd. All rights reserved.

Citation

Marco Ferrara, Fabrizio Fiore, Vincenzo Summa, Cristina Gardelli. Development of 2-pyrrolidinyl-N-methyl pyrimidones as potent and orally bioavailable HIV integrase inhibitors. Bioorganic & medicinal chemistry letters. 2010 Sep 1;20(17):5031-4