Potent and highly selective kappa opioid receptor agonists incorporating chroman- and 2,3-dihydrobenzofuran-based constraints.
Two novel chemical classes of kappa opioid receptor agonists, chroman-2-carboxamide derivatives and 2,3-dihydrobenzofuran-2-carboxamide derivatives, were synthesized. These agents exhibited high and selective affinity for the kappa opioid receptor.
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
Mike
M
Little
Patrick J
PJ
DeHaven-Hudkins
Diane L
DL
Dolle
Roland E
RE
D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000701:Analgesics, Opioid / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D001572:Benzofurans / Q000737:chemistry; D002839:Chromans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D017473:Receptors, Opioid, kappa / Q000819:agonists*
D000577:Amides; D000701:Analgesics, Opioid; D001572:Benzofurans; D002839:Chromans; D017473:Receptors, Opioid, kappa; C043168:coumaran