Novel malonamide derivatives as potent kappa opioid receptor agonists.
A novel series of malonamide derivatives was synthesized. These amides were shown to be potent and selective kappa opioid receptor agonists.
Chu
Guo-Hua
GH
Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA. ghchu@adolor.com
Gu
Minghua
M
Cassel
Joel A
JA
Belanger
Serge
S
Graczyk
Thomas M
TM
DeHaven
Robert N
RN
Conway-James
Nathalie
N
Koblish
Michael
M
Little
Patrick J
PJ
DeHaven-Hudkins
Diane L
DL
Dolle
Roland E
RE
D002626:Chemistry, Pharmaceutical / Q000379:methods*; D019389:Cytochrome P-450 CYP2D6 / Q000737:chemistry; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008314:Malonates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008956:Models, Chemical; D008968:Molecular Conformation; D017473:Receptors, Opioid, kappa / Q000037:antagonists & inhibitors*
D008314:Malonates; D017473:Receptors, Opioid, kappa; D019389:Cytochrome P-450 CYP2D6; C008314:malonamide