title: Inhibitors of inosine monophosphate dehydrogenase: SARs about the N-[3-Methoxy-4-(5-oxazolyl)phenyl moiety.
abstract: 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.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. iwanowie@bms.com
authors.forename: Edwin J
authors.initials: EJ
authors.lastname: Iwanowicz
authors.forename: Scott H
authors.initials: SH
authors.lastname: Watterson
authors.forename: Junqing
authors.initials: J
authors.lastname: Guo
authors.forename: William J
authors.initials: WJ
authors.lastname: Pitts
authors.forename: T G
authors.initials: TG
authors.lastname: Murali Dhar
authors.forename: Zhongqi
authors.initials: Z
authors.lastname: Shen
authors.forename: Ping
authors.initials: P
authors.lastname: Chen
authors.forename: Henry H
authors.initials: HH
authors.lastname: Gu
authors.forename: Catherine A
authors.initials: CA
authors.lastname: Fleener
authors.forename: Katherine A
authors.initials: KA
authors.lastname: Rouleau
authors.forename: Daniel L
authors.initials: DL
authors.lastname: Cheney
authors.forename: Robert M
authors.initials: RM
authors.lastname: Townsend
authors.forename: Diane L
authors.initials: DL
authors.lastname: Hollenbaugh
mesh_terms: 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
chemical_list: 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