Orally Bioavailable Quinoxaline Inhibitors of 15-Prostaglandin Dehydrogenase (15-PGDH) Promote Tissue Repair and Regeneration

15-Prostaglandin dehydrogenase (15-PGDH) regulates the concentration of prostaglandin E2 in vivo. Inhibitors of 15-PGDH elevate PGE2 levels and promote tissue repair and regeneration. Here, we describe a novel class of quinoxaline amides that show potent inhibition of 15-PGDH, good oral bioavailabil...

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Bibliographic Details
Published in:	Journal of medicinal chemistry Vol. 65; no. 22; pp. 15327 - 15343
Main Authors:	Hu, Bin, Toda, Kosuke, Wang, Xiaoyu, Antczak, Monika I., Smith, Julianne, Geboers, Sophie, Nishikawa, Gen, Li, Hongyun, Dawson, Dawn, Fink, Stephen, Desai, Amar B., Williams, Noelle S., Markowitz, Sanford D., Ready, Joseph M.
Format:	Journal Article
Language:	English
Published:	United States American Chemical Society 24-11-2022
Subjects:	Animals Colitis, Ulcerative - drug therapy Dinoprostone Hydroxyprostaglandin Dehydrogenases - antagonists & inhibitors Mice Quinoxalines - pharmacology
Online Access:	Get full text
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Summary:	15-Prostaglandin dehydrogenase (15-PGDH) regulates the concentration of prostaglandin E2 in vivo. Inhibitors of 15-PGDH elevate PGE2 levels and promote tissue repair and regeneration. Here, we describe a novel class of quinoxaline amides that show potent inhibition of 15-PGDH, good oral bioavailability, and protective activity in mouse models of ulcerative colitis and recovery from bone marrow transplantation.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0022-2623 1520-4804
DOI:	10.1021/acs.jmedchem.2c01299