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

• Published in: Bioorganic & medicinal chemistry letters Vol. 13; no. 3; pp. 543 - 546
• Main Authors: 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: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 10.02.2003; Elsevier
• Subjects: 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; Five membered ring; Enzyme; Nitrogen heterocycle; Isozyme; IMP dehydrogenase; Enzyme inhibitor; Quinoline derivatives; In vitro; Thiophene derivatives; Sulfur heterocycle; Structure activity relation; T-Lymphocyte; Bicyclic compound; Aromatic compound; Oxidoreductases; Chemical synthesis; Oxazole derivatives; Oxygen nitrogen heterocycle
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/S0960-894X(02)00944-7

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.