title: 3-Aryl-4-hydroxyquinolin-2(1H)-one derivatives as type I fatty acid synthase inhibitors.
abstract: A series of 3-aryl-4-hydroxyquinolin-2(1H)-ones with fatty acid synthase inhibitory activity was prepared. Starting from a derivative with an IC(50) = 1.4 microM, SAR studies led to compounds with more than 70-fold increase in potency (IC(50) < 20 nM).
authors.affiliation: Department of Chemistry, Merck Research Laboratories, Boston, MA 02115, USA. alexey_rivkin@merck.com
authors.forename: Alexey
authors.initials: A
authors.lastname: Rivkin
authors.forename: Yoona R
authors.initials: YR
authors.lastname: Kim
authors.forename: Mark T
authors.initials: MT
authors.lastname: Goulet
authors.forename: Nathan
authors.initials: N
authors.lastname: Bays
authors.forename: Armetta D
authors.initials: AD
authors.lastname: Hill
authors.forename: Ilona
authors.initials: I
authors.lastname: Kariv
authors.forename: Stefan
authors.initials: S
authors.lastname: Krauss
authors.forename: Nicole
authors.initials: N
authors.lastname: Ginanni
authors.forename: Peter R
authors.initials: PR
authors.lastname: Strack
authors.forename: Nancy E
authors.initials: NE
authors.lastname: Kohl
authors.forename: Christine C
authors.initials: CC
authors.lastname: Chung
authors.forename: Jeffrey P
authors.initials: JP
authors.lastname: Varnerin
authors.forename: Paul N
authors.initials: PN
authors.lastname: Goudreau
authors.forename: Amy
authors.initials: A
authors.lastname: Chang
authors.forename: Michael R
authors.initials: MR
authors.lastname: Tota
authors.forename: Benito
authors.initials: B
authors.lastname: Munoz
mesh_terms: D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D064429:Fatty Acid Synthases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D006912:Hydroxyquinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008314:Malonates / Q000737:chemistry; D008872:Microwaves; D015394:Molecular Structure; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D006912:Hydroxyquinolines; D008314:Malonates; D011804:Quinolines; D064429:Fatty Acid Synthases