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

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. The preparation and in vitro biological evaluation of a novel series of...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-02, Vol.13 (3), p.543-546
Hauptverfasser:	Watterson, Scott H., Carlsen, Marianne, Murali Dhar, T.G., Shen, Zhongqi, Pitts, William J., Guo, Junqing, Gu, Henry H., Norris, Derek, Chorba, John, Chen, Ping, Cheney, Daniel, Witmer, Mark, Fleener, Catherine A., Rouleau, Katherine, Townsend, Robert, Hollenbaugh, Diane L., Iwanowicz, Edwin J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences 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 Medical sciences Miscellaneous Pharmacology. Drug treatments Quinolones - chemical synthesis Quinolones - pharmacology Structure-Activity Relationship T-Lymphocytes - drug effects T-Lymphocytes - enzymology
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Zusammenfassung:	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. The preparation and in vitro biological evaluation of a novel series of potent, selective quinolone-based small molecule inhibitors of IMPDH are described.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(02)00944-7