A survey of cyclic replacements for the central diamide moiety of inhibitors of inosine monophosphate dehydrogenase.
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.
Dhar
T G Murali
TG
Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. dharm@bms.com
Liu
Chunjian
C
Pitts
William J
WJ
Guo
Junquing
J
Watterson
Scott H
SH
Gu
Henry
H
Fleener
Catherine A
CA
Rouleau
Katherine
K
Sherbina
N Z
NZ
Barrish
Joel C
JC
Hollenbaugh
Diane
D
Iwanowicz
Edwin J
EJ
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
D004791:Enzyme Inhibitors; D006571:Heterocyclic Compounds; D007202:Indicators and Reagents; D008024:Ligands; D007168:IMP Dehydrogenase