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

By Ferrara, Marco; Fiore, Fabrizio; Summa, Vincenzo; Gardelli, Cristina
From Bioorganic & Medicinal Chemistry Letters (2010), 20(17), 5031-5034. Language: English, Database: CAPLUS, DOI:10.1016/j.bmcl.2010.07.042

A series of 2-pyrrolidinyl-N-Me pyrimidones HIV integrase inhibitors has been explored leading to the identification of deriv. 13, which showed high activity at inhibiting viral replication in cell culture, favorable pharmacokinetic profile in two preclin. species, and an attractive profile against a panel of HIV-integrase mutants.