A survey of cyclic replacements for the central diamide moiety of inhibitors of inosine monophosphate dehydrogenase

T G Murali Dhar; Chunjian Liu; William J Pitts; Junquing Guo; Scott H Watterson; Henry Gu; Catherine A Fleener; Katherine Rouleau; N Z Sherbina; Joel C Barrish; Diane Hollenbaugh; Edwin J Iwanowicz

doi:10.1016/s0960-894x(02)00641-8

A survey of cyclic replacements for the central diamide moiety of inhibitors of inosine monophosphate dehydrogenase

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3125-8. doi: 10.1016/s0960-894x(02)00641-8.

Authors

T G Murali Dhar¹, Chunjian Liu, William J Pitts, Junquing Guo, Scott H Watterson, Henry Gu, Catherine A Fleener, Katherine Rouleau, N Z Sherbina, Joel C Barrish, Diane Hollenbaugh, Edwin J Iwanowicz

Affiliation

¹ Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. [email protected]

PMID: 12372516
DOI: 10.1016/s0960-894x(02)00641-8

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.

MeSH terms

Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology*
Heterocyclic Compounds / chemical synthesis*
Heterocyclic Compounds / pharmacology*
Humans
IMP Dehydrogenase / antagonists & inhibitors*
In Vitro Techniques
Indicators and Reagents
Ligands
Lymphocytes / drug effects
Lymphocytes / metabolism
Models, Molecular
Molecular Conformation
Stereoisomerism
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Heterocyclic Compounds
Indicators and Reagents
Ligands
IMP Dehydrogenase