title: Identification and characterization of amino-piperidinequinolones and quinazolinones as MCHr1 antagonists.
abstract: Several potent, functionally active MCHr1 antagonists derived from quinolin-2(1H)-ones and quinazoline-2(1H)-ones have been synthesized and evaluated. Pyridylmethyl substitution at the quinolone 1-position results in derivatives with low-nM binding potency and good selectivity with respect to hERG binding.
authors.affiliation: Millennium Pharmaceuticals, Inc., 40 Landsdowne St. Cambridge, MA 02139, USA. chris.blackburn@mpi.com
authors.forename: Christopher
authors.initials: C
authors.lastname: Blackburn
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: LaMarche
authors.forename: James
authors.initials: J
authors.lastname: Brown
authors.forename: Jennifer Lee
authors.initials: JL
authors.lastname: Che
authors.forename: Courtney A
authors.initials: CA
authors.lastname: Cullis
authors.forename: Sujen
authors.initials: S
authors.lastname: Lai
authors.forename: Martin
authors.initials: M
authors.lastname: Maguire
authors.forename: Thomas
authors.initials: T
authors.lastname: Marsilje
authors.forename: Bradley
authors.initials: B
authors.lastname: Geddes
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Govek
authors.forename: Vivek
authors.initials: V
authors.lastname: Kadambi
authors.forename: Colleen
authors.initials: C
authors.lastname: Doherty
authors.forename: Brian
authors.initials: B
authors.lastname: Dayton
authors.forename: Sevan
authors.initials: S
authors.lastname: Brodjian
authors.forename: Kennan C
authors.initials: KC
authors.lastname: Marsh
authors.forename: Christine A
authors.initials: CA
authors.lastname: Collins
authors.forename: Philip R
authors.initials: PR
authors.lastname: Kym
mesh_terms: D000818:Animals; D051379:Mice; D011799:Quinazolines / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D015363:Quinolones / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D011979:Receptors, Pituitary Hormone / Q000037:antagonists & inhibitors*
chemical_list: D011799:Quinazolines; D015363:Quinolones; D011979:Receptors, Pituitary Hormone; C092274:melanin-concentrating hormone receptor