title: Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1.
abstract: A high-throughput screen was performed in order to identify chemotypes that are bound by the melanin concentrating hormone receptor-1 (MCHr1). A novel 2-amino-8-alkoxyquinoline compound (1) was identified and subsequently optimized using a parallel and automated procedure for the rapid production of multiple analogs. The structure-activity relationships that emerged from this effort are described, along with selected pharmacokinetic parameters of compound (d)-61 when dosed orally in diet-induced obese mice.
authors.affiliation: Metabolic Diseases Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA. andrew.souers@abbott.com
authors.forename: Andrew J
authors.initials: AJ
authors.lastname: Souers
authors.forename: Dariusz
authors.initials: D
authors.lastname: Wodka
authors.forename: Ju
authors.initials: J
authors.lastname: Gao
authors.forename: Jared C
authors.initials: JC
authors.lastname: Lewis
authors.forename: Anil
authors.initials: A
authors.lastname: Vasudevan
authors.forename: Robert
authors.initials: R
authors.lastname: Gentles
authors.forename: Sevan
authors.initials: S
authors.lastname: Brodjian
authors.forename: Brian
authors.initials: B
authors.lastname: Dayton
authors.forename: Christopher A
authors.initials: CA
authors.lastname: Ogiela
authors.forename: Dennis
authors.initials: D
authors.lastname: Fry
authors.forename: Lisa E
authors.initials: LE
authors.lastname: Hernandez
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; D019440:Anti-Obesity Agents / Q000138:chemical synthesis*; D051379:Mice; D011804:Quinolines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D019440:Anti-Obesity Agents; C491209:Mchr1 protein, mouse; D011804:Quinolines; D017481:Receptors, Somatostatin