Novel inhibitors of IMPDH: a highly potent and selective quinolone-based series.
A series of novel quinolone-based small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH) was explored. The synthesis and the structure-activity relationships (SARs) derived from in vitro studies are described.
Watterson
Scott H
SH
Bristol-Myers Squibb PRI, PO Box 400, Princeton, NJ 08543-4000, USA. scott.waterson@bms.com
Carlsen
Marianne
M
Dhar
T G Murali
TG
Shen
Zhongqi
Z
Pitts
William J
WJ
Guo
Junqing
J
Gu
Henry H
HH
Norris
Derek
D
Chorba
John
J
Chen
Ping
P
Cheney
Daniel
D
Witmer
Mark
M
Fleener
Catherine A
CA
Rouleau
Katherine
K
Townsend
Robert
R
Hollenbaugh
Diane L
DL
Iwanowicz
Edwin J
EJ
D002455:Cell Division / Q000187:drug effects; D002478:Cells, Cultured; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D007168:IMP Dehydrogenase / Q000037:antagonists & inhibitors*; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013601:T-Lymphocytes / Q000187:drug effects / Q000201:enzymology
D004791:Enzyme Inhibitors; D015363:Quinolones; D007168:IMP Dehydrogenase