title: Tricyclic HIV integrase inhibitors: potent and orally bioavailable C5-aza analogs.
abstract: A series of C5-aza tricyclic HIV integrase inhibitors was prepared. A highly potent and orally bioavailable compound (compound 9) was identified and selected for development.
authors.affiliation: Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
authors.forename: Haolun
authors.initials: H
authors.lastname: Jin
authors.forename: Matthew
authors.initials: M
authors.lastname: Wright
authors.forename: Richard
authors.initials: R
authors.lastname: Pastor
authors.forename: Michael
authors.initials: M
authors.lastname: Mish
authors.forename: Sammy
authors.initials: S
authors.lastname: Metobo
authors.forename: Salman
authors.initials: S
authors.lastname: Jabri
authors.forename: Rachael
authors.initials: R
authors.lastname: Lansdown
authors.forename: Ruby
authors.initials: R
authors.lastname: Cai
authors.forename: Peter
authors.initials: P
authors.lastname: Pyun
authors.forename: Manuel
authors.initials: M
authors.lastname: Tsiang
authors.forename: Xiaowu
authors.initials: X
authors.lastname: Chen
authors.forename: Choung U
authors.initials: CU
authors.lastname: Kim
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001374:Azacitidine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D001682:Biological Availability; D018360:Crystallography, X-Ray; D004285:Dogs; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D009930:Organic Chemicals / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D011760:Pyrrolidinones; D000068898:Raltegravir Potassium; D051381:Rats
chemical_list: D019428:HIV Integrase Inhibitors; D009930:Organic Chemicals; D011760:Pyrrolidinones; D000068898:Raltegravir Potassium; D001374:Azacitidine