Pyridine-3-carboxamides as novel CB(2) agonists for analgesia.
We describe herein the medicinal chemistry approach which led to the discovery of a novel pyridine-3-carboxamide series of CB(2) receptor agonists. The SAR of this new template was evaluated and culminated in the identification of analogue 14a which demonstrated efficacy in an in vivo model of inflammatory pain.
Mitchell
William L
WL
GlaxoSmithKline PLC, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Third Avenue, Harlow, Essex, UK. bill.mitchell777@tiscali.co.uk
Giblin
Gerard M P
GM
Naylor
Alan
A
Eatherton
Andrew J
AJ
Slingsby
Brian P
BP
Rawlings
Anthony D
AD
Jandu
Karamjit S
KS
Haslam
Carl P
CP
Brown
Andrew J
AJ
Goldsmith
Paul
P
Clayton
Nick M
NM
Wilson
Alex W
AW
Chessell
Iain P
IP
Green
Richard H
RH
Whittington
Andrew R
AR
Wall
Ian D
ID
D000577:Amides / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D000698:Analgesia / Q000379:methods; D000700:Analgesics / Q000138:chemical synthesis*; D000818:Animals; D004195:Disease Models, Animal; D055808:Drug Discovery / Q000379:methods; D007249:Inflammation; D010146:Pain / Q000188:drug therapy; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use*; D043885:Receptor, Cannabinoid, CB2 / Q000819:agonists*; D013329:Structure-Activity Relationship
D000577:Amides; D000700:Analgesics; D011725:Pyridines; D043885:Receptor, Cannabinoid, CB2