The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis. Issue 9 (1st May 2017)

• Record Type: Journal Article
• Authors: Liddle, John; Beaufils, Benjamin; Binnie, Margaret; Bouillot, Anne; Denis, Alexis A.; Hann, Michael M.; Haslam, Carl P.; Holmes, Duncan S.; Hutchinson, Jon P.; Kranz, Michael; McBride, Andrew; Mirguet, Olivier; Mole, Damian J.; Mowat, Christopher G.; Pal, Sandeep; Rowland, Paul; Trottet, Lionel; Uings, Iain J.; Walker, Ann L.; Webster, Scott P.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 9(2017)
• Page Start: 2023
• Page End: 2028
• Publication Date: 2017-05-01
• Subjects: Kynurenine -- Monooxygenase -- Tryptophan -- Substrate -- Pancreatitis; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.02.078
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A series of potent, competitive and highly selective kynurenine monooxygenase inhibitors have been discovered via a substrate-based approach for the treatment of acute pancreatitis. The lead compound demonstrated good cellular potency and clear pharmacodynamic activity in vivo .