title: Synthesis and HIV-integrase strand transfer inhibition activity of 7-hydroxy[1,3]thiazolo[5,4-b]pyridin-5(4H)-ones.
abstract: An efficient synthesis of methyl 7-hydroxy[1,3]thiazolo[5,4-b]pyridin-5(4H)-one-6-carboxylates (8-10 and 16) and 6-carboxamides (17-20) is described. Sub-micromolar enzyme inhibition of HIV integrase was achieved with several carboxamide analogs which were superior to their carboxylic ester congeners.
authors.affiliation: GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, NC 27709, USA. eric.e.boros@gsk.com
authors.forename: Eric E
authors.initials: EE
authors.lastname: Boros
authors.forename: Brian A
authors.initials: BA
authors.lastname: Johns
authors.forename: Edward P
authors.initials: EP
authors.lastname: Garvey
authors.forename: Cecilia S
authors.initials: CS
authors.lastname: Koble
authors.forename: Wayne H
authors.initials: WH
authors.lastname: Miller
mesh_terms: D006678:HIV / Q000201:enzymology*; D019427:HIV Integrase; D019428:HIV Integrase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D007659:Ketones / Q000737:chemistry / Q000494:pharmacology*; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology*; D013844:Thiazoles / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D019428:HIV Integrase Inhibitors; D007659:Ketones; D011725:Pyridines; D013844:Thiazoles; D019427:HIV Integrase