title: Development of 2-t butyl-N-methyl pyrimidones as potent inhibitors of HIV integrase.
abstract: A series of novel 2-(t)butyl-N-methyl pyrimidone HIV-1 integrase inhibitors have been identified. Optimization of the initial lead resulted in compounds such as 9d and 14a, which showed high levels of activity in cell culture inhibiting viral replication with CIC(95) of 10nM in the presence of 50% normal human serum.
authors: Department of Medicinal Chemistry, IRBM-MRL Rome, Via Pontina, Km 30.600, 00040 Pomezia, Rome, Italy. mariaemilia_difrancesco@merck.com
authors: M Emilia
authors: ME
authors: Di Francesco
authors: Paola
authors: P
authors: Pace
authors: Fabrizio
authors: F
authors: Fiore
authors: Francesca
authors: F
authors: Naimo
authors: Fabio
authors: F
authors: Bonelli
authors: Michael
authors: M
authors: Rowley
authors: Vincenzo
authors: V
authors: Summa
mesh_terms: D000577:Amides / Q000737:chemistry; D000818:Animals; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008745:Methylation; D015394:Molecular Structure; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D019428:HIV Integrase Inhibitors; D011744:Pyrimidinones