title: A survey of cyclic replacements for the central diamide moiety of inhibitors of inosine monophosphate dehydrogenase.
abstract: A series of heterocyclic replacements for the central diamide moiety of 1, a potent small molecule inhibitor of inosine monophosphate dehydrogenase (IMPDH) were explored The synthesis and the structure-activity relationships (SARs), derived from in vitro studies, for these new series of inhibitors is given.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. dharm@bms.com
authors.forename: T G Murali
authors.initials: TG
authors.lastname: Dhar
authors.forename: Chunjian
authors.initials: C
authors.lastname: Liu
authors.forename: William J
authors.initials: WJ
authors.lastname: Pitts
authors.forename: Junquing
authors.initials: J
authors.lastname: Guo
authors.forename: Scott H
authors.initials: SH
authors.lastname: Watterson
authors.forename: Henry
authors.initials: H
authors.lastname: Gu
authors.forename: Catherine A
authors.initials: CA
authors.lastname: Fleener
authors.forename: Katherine
authors.initials: K
authors.lastname: Rouleau
authors.forename: N Z
authors.initials: NZ
authors.lastname: Sherbina
authors.forename: Joel C
authors.initials: JC
authors.lastname: Barrish
authors.forename: Diane
authors.initials: D
authors.lastname: Hollenbaugh
authors.forename: Edwin J
authors.initials: EJ
authors.lastname: Iwanowicz
mesh_terms: D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D007168:IMP Dehydrogenase / Q000037:antagonists & inhibitors*; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D008024:Ligands; D008214:Lymphocytes / Q000187:drug effects / Q000378:metabolism; D008958:Models, Molecular; D008968:Molecular Conformation; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D006571:Heterocyclic Compounds; D007202:Indicators and Reagents; D008024:Ligands; D007168:IMP Dehydrogenase