Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists.
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.
Sasmal
Pradip K
PK
Discovery Research, Dr. Reddy's Laboratories Ltd, Bollaram Road, Miyapur, Hyderabad 500 049, India. sasmalpk@yahoo.co.in
Sasmal
Sanjita
S
Rao
P Tirumala
PT
Venkatesham
B
B
Roshaiah
M
M
Abbineni
Chandrasekhar
C
Khanna
Ish
I
Jadhav
Vikram P
VP
Suresh
J
J
Talwar
Rashmi
R
Muzeeb
Syed
S
Receveur
Jean-Marie
JM
Frimurer
Thomas M
TM
Rist
Øystein
Ø
Elster
Lisbeth
L
Högberg
Thomas
T
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
D019440:Anti-Obesity Agents; D001562:Benzimidazoles; C103263:MCHR1 protein, human; D017481:Receptors, Somatostatin