Development of 2-pyrrolidinyl-N-methyl pyrimidones as potent and orally bioavailable HIV integrase inhibitors.
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.
Ferrara
Marco
M
Department of Medicinal Chemistry IRBM-MRL, Pomezia (RM), Italy. marco.ferrara@boehringer-ingelheim.com
Fiore
Fabrizio
F
Summa
Vincenzo
V
Gardelli
Cristina
C
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
D019428:HIV Integrase Inhibitors; D011744:Pyrimidinones