Aminopyridinecarboxamide-based inhibitors: Structure-activity relationship.
Series of aminopyridinecarboxamide-based inhibitors were synthesized and tested against human recombinant IKK-2 and in IL-1beta stimulated synovial fibroblasts. The 2-amino-5-chloropyridine-4-carboxamides were identified as the most potent inhibitors with improved cellular activity.
Bonafoux
Dominique F
DF
Department of Medicinal Chemistry, Pfizer Inc, 700 Chesterfield Parkway West, St Louis, MO 63017, United States. dominique.bonafoux@abbott.com
Bonar
Sheri L
SL
Clare
Michael
M
Donnelly
Ann M
AM
Glaenzer
Jeanette L
JL
Guzova
Julia A
JA
Huang
He
H
Kishore
Nandidni N
NN
Koszyk
Francis J
FJ
Lennon
Patrick J
PJ
Libby
Adam
A
Mathialagan
Sumathy
S
Oburn
David S
DS
Rouw
Sharon A
SA
Sommers
Cynthia D
CD
Tripp
Catherine S
CS
Vanella
Lori J
LJ
Weier
Richard
R
Wolfson
Serge G
SG
Huang
Horng-Chih
HC
D000577:Amides / Q000737:chemistry / Q000494:pharmacology; D000595:Amino Acid Sequence; D000632:Aminopyrine / Q000737:chemistry* / Q000494:pharmacology*; D000893:Anti-Inflammatory Agents / Q000737:chemistry* / Q000494:pharmacology*; D001172:Arthritis, Rheumatoid / Q000188:drug therapy; D005347:Fibroblasts / Q000187:drug effects / Q000276:immunology; D006801:Humans; D051550:I-kappa B Kinase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D020672:I-kappa B Proteins / Q000737:chemistry; D053583:Interleukin-1beta / Q000037:antagonists & inhibitors* / Q000378:metabolism; D017746:Joint Capsule / Q000166:cytology; D008969:Molecular Sequence Data; D013329:Structure-Activity Relationship
D000577:Amides; D000893:Anti-Inflammatory Agents; C083487:I kappa B beta protein; D020672:I-kappa B Proteins; D053583:Interleukin-1beta; D000632:Aminopyrine; D051550:I-kappa B Kinase