New amide derivatives as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.
Melanin-concentrating hormone (MCH) is a recently discovered central nervous system (CNS) target for treating obesity. Two novel series of amide derivatives were synthesized and evaluated biologically as MCH-R1 (melanin-concentrating hormone receptor 1) antagonists. The results showed that diphenyl substituents on the amide lead to better activity than biphenyl substituents.
Cirauqui
Nuria
N
Unidad de Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), University of Navarra, Pamplona, Spain.
Ceras
Javier
J
Galiano
Silvia
S
Pérez-Silanes
Silvia
S
Juanenea
Laura
L
Rivera
Gildardo
G
Aldana
Ignacio
I
Monge
Antonio
A
D000577:Amides / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D019440:Anti-Obesity Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans; D007202:Indicators and Reagents; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors*; D012997:Solvents; D013329:Structure-Activity Relationship
D000577:Amides; D019440:Anti-Obesity Agents; D007202:Indicators and Reagents; C103263:MCHR1 protein, human; D017481:Receptors, Somatostatin; D012997:Solvents