Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists.
Several potent and efficacious MCHr1 antagonists containing an ortho-amino benzamide or nicotinamide chemotype have been identified, exemplified by 28 and 50.
Vasudevan
Anil
A
Metabolic Diseases Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA. Anil.Vasudevan@abbott.com
LaMarche
Matthew J
MJ
Blackburn
Christopher
C
Che
Jennifer Lee
JL
Luchaco-Cullis
Courtney A
CA
Lai
Sujen
S
Marsilje
Thomas H
TH
Patane
Michael A
MA
Souers
Andrew J
AJ
Wodka
Derek
D
Geddes
Bradley
B
Chen
Sumiao
S
Brodjian
Seven
S
Falls
Doug H
DH
Dayton
Brian D
BD
Bush
Eugene
E
Brune
Michael
M
Shapiro
Robin D
RD
Marsh
Kennan C
KC
Hernandez
Lisa E
LE
Sham
Hing L
HL
Collins
Christine A
CA
Kym
Philip R
PR
D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D051379:Mice; D008815:Mice, Inbred Strains; D009536:Niacinamide / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology; D010599:Pharmacokinetics; D017481:Receptors, Somatostatin / Q000819:agonists / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014018:Tissue Distribution; D062367:ortho-Aminobenzoates / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology
D001549:Benzamides; C491209:Mchr1 protein, mouse; D017481:Receptors, Somatostatin; D062367:ortho-Aminobenzoates; D009536:Niacinamide