Inhibitors of inosine monophosphate dehydrogenase: SARs about the N-[3-Methoxy-4-(5-oxazolyl)phenyl moiety.
The first reported structure-activity relationships (SARs) about the N-[3-methoxy-4-(5-oxazolyl)phenyl moiety for a series of recently disclosed inosine monophosphate dehydrogenase (IMPDH) inhibitors are described. The syntheses and in vitro inhibitory values for IMPDH II, and T-cell proliferation (for select analogues) are given.
Iwanowicz
Edwin J
EJ
Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. iwanowie@bms.com
Watterson
Scott H
SH
Guo
Junqing
J
Pitts
William J
WJ
Murali Dhar
T G
TG
Shen
Zhongqi
Z
Chen
Ping
P
Gu
Henry H
HH
Fleener
Catherine A
CA
Rouleau
Katherine A
KA
Cheney
Daniel L
DL
Townsend
Robert M
RM
Hollenbaugh
Diane L
DL
D000818:Animals; D002219:Carbamates / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D006224:Cricetinae; D003412:Cricetulus; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D007168:IMP Dehydrogenase / Q000037:antagonists & inhibitors*; D020128:Inhibitory Concentration 50; D008213:Lymphocyte Activation / Q000187:drug effects; D009173:Mycophenolic Acid / Q000031:analogs & derivatives / Q000494:pharmacology; D010080:Oxazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D010671:Phenylurea Compounds / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013601:T-Lymphocytes / Q000187:drug effects / Q000502:physiology
D002219:Carbamates; D004791:Enzyme Inhibitors; C407002:N-3-(3-(3-methoxy-4-oxazol-5-ylphenyl)ureido)benzylcarbamic acid tetrahydrofuran-3-yl ester; D010080:Oxazoles; D010671:Phenylurea Compounds; D007168:IMP Dehydrogenase; D009173:Mycophenolic Acid