title: Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists.
abstract: Melanin concentrating hormone (MCH) is an important mediator of energy homeostasis and plays role in several disorders such as obesity, stress, depression and anxiety. The synthesis and biological evaluation of novel benzimidazole derivatives as MCHR1 antagonists are described. The in vivo proof of principle for weight loss with a lead compound from this series is exemplified.
authors: Discovery Research, Dr. Reddy's Laboratories Ltd, Bollaram Road, Miyapur, Hyderabad 500 049, India. sasmalpk@yahoo.co.in
authors: Pradip K
authors: PK
authors: Sasmal
authors: Sanjita
authors: S
authors: Sasmal
authors: P Tirumala
authors: PT
authors: Rao
authors: B
authors: B
authors: Venkatesham
authors: M
authors: M
authors: Roshaiah
authors: Chandrasekhar
authors: C
authors: Abbineni
authors: Ish
authors: I
authors: Khanna
authors: Vikram P
authors: VP
authors: Jadhav
authors: J
authors: J
authors: Suresh
authors: Rashmi
authors: R
authors: Talwar
authors: Syed
authors: S
authors: Muzeeb
authors: Jean-Marie
authors: JM
authors: Receveur
authors: Thomas M
authors: TM
authors: Frimurer
authors: Øystein
authors: Ø
authors: Rist
authors: Lisbeth
authors: L
authors: Elster
authors: Thomas
authors: T
authors: Högberg
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D051379:Mice; D008810:Mice, Inbred C57BL; D008958:Models, Molecular; D009765:Obesity / Q000188:drug therapy*; D011485:Protein Binding; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D015431:Weight Loss / Q000187:drug effects
chemical_list: D019440:Anti-Obesity Agents; D001562:Benzimidazoles; C103263:MCHR1 protein, human; D017481:Receptors, Somatostatin