Novel inhibitors of IMPDH: a highly potent and selective quinolone-based series

Scott H Watterson; Marianne Carlsen; T G Murali Dhar; Zhongqi Shen; William J Pitts; Junqing Guo; Henry H Gu; Derek Norris; John Chorba; Ping Chen; Daniel Cheney; Mark Witmer; Catherine A Fleener; Katherine Rouleau; Robert Townsend; Diane L Hollenbaugh; Edwin J Iwanowicz

doi:10.1016/s0960-894x(02)00944-7

Novel inhibitors of IMPDH: a highly potent and selective quinolone-based series

Bioorg Med Chem Lett. 2003 Feb 10;13(3):543-6. doi: 10.1016/s0960-894x(02)00944-7.

Authors

Scott H Watterson¹, Marianne Carlsen, T G Murali Dhar, Zhongqi Shen, William J Pitts, Junqing Guo, Henry H Gu, Derek Norris, John Chorba, Ping Chen, Daniel Cheney, Mark Witmer, Catherine A Fleener, Katherine Rouleau, Robert Townsend, Diane L Hollenbaugh, Edwin J Iwanowicz

Affiliation

¹ Bristol-Myers Squibb PRI, PO Box 400, Princeton, NJ 08543-4000, USA. scott.waterson@bms.com

PMID: 12565968
DOI: 10.1016/s0960-894x(02)00944-7

Abstract

A series of novel quinolone-based small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH) was explored. The synthesis and the structure-activity relationships (SARs) derived from in vitro studies are described.

MeSH terms

Cell Division / drug effects
Cells, Cultured
Chemical Phenomena
Chemistry, Physical
Crystallography, X-Ray
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology*
Humans
IMP Dehydrogenase / antagonists & inhibitors*
Quinolones / chemical synthesis*
Quinolones / pharmacology*
Structure-Activity Relationship
T-Lymphocytes / drug effects
T-Lymphocytes / enzymology

Substances

Enzyme Inhibitors
Quinolones
IMP Dehydrogenase