2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists.
A series of 2-aminoquinoline compounds was prepared and evaluated in MCH1R binding and functional antagonist assays. Small dialkyl, methylalkyl, methylcycloalkyl, and cyclic amines were tolerated at the quinoline 2-position. The in vivo efficacy of compound 12 was explored and compared to that of a related inactive analog to determine their effects on food intake and body weight in rodents.
Jiang
Jinlong
J
Department of Medicinal Chemistry, PO Box 2000, Rahway, NJ 07065-0900, USA.
Hoang
Myle
M
Young
Jonathan R
JR
Chaung
Danny
D
Eid
Ronsar
R
Turner
Cherilyn
C
Lin
Peter
P
Tong
Xinchun
X
Wang
Junying
J
Tan
Carina
C
Feighner
Scott
S
Palyha
Oksana
O
Hreniuk
Donna L
DL
Pan
Jie
J
Sailer
Andreas W
AW
MacNeil
Douglas J
DJ
Howard
Andrew
A
Shearman
Lauren
L
Stribling
Sloan
S
Camacho
Ramon
R
Strack
Alison
A
Van der Ploeg
Lex H T
LH
Goulet
Mark T
MT
DeVita
Robert J
RJ
D000818:Animals; D001667:Binding, Competitive; D001681:Biological Assay; D004435:Eating; D004734:Energy Metabolism / Q000187:drug effects; D006801:Humans; D008297:Male; D015394:Molecular Structure; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011812:Quinuclidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000235:genetics; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
C515121:6-(12-(2-fluoromethylpyridin-5-yl)dodecanamido)-2-(1-quinuclidinyl)quinoline; C103263:MCHR1 protein, human; C491208:MCHR1 protein, rat; D011804:Quinolines; D011812:Quinuclidines; D017481:Receptors, Somatostatin