Search

Your search keyword '"Diane L, Hollenbaugh"' showing total 2 results
Start Over Author "Diane L, Hollenbaugh" Topic enzyme inhibitors
2 results on '"Diane L, Hollenbaugh"'

1. Discovery of N-[2-[2-[[3-Methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a Novel and Potent Inhibitor of Inosine Monophosphate Dehydrogenase with Excellent in Vivo Activity

Author

T G Murali, Dhar, Zhongqi, Shen, Junqing, Guo, Chunjian, Liu, Scott H, Watterson, Henry H, Gu, William J, Pitts, Catherine A, Fleener, Katherine A, Rouleau, N Z, Sherbina, Kim W, McIntyre, David J, Shuster, Mark R, Witmer, Jeffrey A, Tredup, Bang-Chi, Chen, Rulin, Zhao, Mark S, Bednarz, Daniel L, Cheney, John F, MacMaster, Laura M, Miller, Karen K, Berry, Timothy W, Harper, Joel C, Barrish, Diane L, Hollenbaugh, and Edwin J, Iwanowicz

Subjects
Male, Purine, Stereochemistry, Morpholines, Enzyme-Linked Immunosorbent Assay, Chemical synthesis, Mice, Structure-Activity Relationship, chemistry.chemical_compound, IMP Dehydrogenase, In vivo, IMP dehydrogenase, Drug Discovery, Animals, Structure–activity relationship, Nucleotide, Enzyme Inhibitors, Oxazoles, chemistry.chemical_classification, Mice, Inbred BALB C, biology, Mycophenolic Acid, Arthritis, Experimental, Rats, De novo synthesis, Biochemistry, chemistry, Rats, Inbred Lew, Enzyme inhibitor, Antibody Formation, biology.protein, Molecular Medicine
Abstract

Inosine monophosphate dehydrogenase (IMPDH) is a key enzyme that is involved in the de novo synthesis of purine nucleotides. Novel 2-aminooxazoles were synthesized and tested for inhibition of IMPDH catalytic activity. Multiple analogues based on this chemotype were found to inhibit IMPDH with low nanomolar potency. One of the analogues (compound 23) showed excellent in vivo activity in the inhibition of antibody production in mice and in the adjuvant induced arthritis model in rats.

Published
2002
Full Text
View/download PDF

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

Author

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, and Edwin J, Iwanowicz

Subjects
Structure-Activity Relationship, IMP Dehydrogenase, Chemical Phenomena, Chemistry, Physical, T-Lymphocytes, Humans, Enzyme Inhibitors, Quinolones, Crystallography, X-Ray, Cell Division, Cells, Cultured
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.

Published
2003

Catalog

Books, media, physical & digital resources
See catalog results