title: Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists.
abstract: We report here new chemical series acting as antagonists of melanin-concentrating hormone receptor 1 (MCHR-1). Synthesis and structure-activity relationships are described leading to the identification of compounds with optimized in vitro pharmacological and in vitro ADME profiles. In vivo activity has been demonstrated in animal models of food intake and depression.
authors: Cerep, 19 avenue du Québec Courtaboeuf 1, 91951 Villebon sur Yvette, France. fabrice.balavoine@quantum-genomics.com <fabrice.balavoine@quantum-genomics.com>
authors: Fabrice
authors: F
authors: Balavoine
authors: Patrice
authors: P
authors: Malabre
authors: Thierry
authors: T
authors: Alleaume
authors: Astrid
authors: A
authors: Rey
authors: Valérie
authors: V
authors: Cherfils
authors: Olivier
authors: O
authors: Jeanneton
authors: Sophie
authors: S
authors: Seigneurin-Venin
authors: Frédéric
authors: F
authors: Revah
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003863:Depression / Q000188:drug therapy; D004195:Disease Models, Animal; D015195:Drug Design; D005247:Feeding Behavior / Q000187:drug effects; D006827:Hydantoins / Q000737:chemistry*; D007700:Kinetics; D008543:Melanins / Q000737:chemistry*; D008954:Models, Biological; D008956:Models, Chemical; D008958:Models, Molecular; D011979:Receptors, Pituitary Hormone / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D006827:Hydantoins; D008543:Melanins; D011979:Receptors, Pituitary Hormone; D017481:Receptors, Somatostatin; C092274:melanin-concentrating hormone receptor