title: Development of 2-pyrrolidinyl-N-methyl pyrimidones as potent and orally bioavailable HIV integrase inhibitors.
abstract: 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.
authors.affiliation: Department of Medicinal Chemistry IRBM-MRL, Pomezia (RM), Italy. marco.ferrara@boehringer-ingelheim.com
authors.forename: Marco
authors.initials: M
authors.lastname: Ferrara
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Fiore
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Summa
authors.forename: Cristina
authors.initials: C
authors.lastname: Gardelli
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D019428:HIV Integrase Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D011744:Pyrimidinones / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats
chemical_list: D019428:HIV Integrase Inhibitors; D011744:Pyrimidinones