The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis

John Liddle,Benjamin Beaufils,Margaret Binnie,Anne Marie Jeanne Bouillot,Alexis Denis,Michael M. Hann,Carl Haslam,Duncan S. Holmes, Jon P. Hutchinson,Michael Kranz,Andrew McBride,Olivier Mirguet,Damian J. Mole,Christopher G. Mowat,Sandeep Pal,Paul Rowland,Lionel Trottet,Iain Uings,Ann Louise Walker,Scott P. Webster

Bioorganic & Medicinal Chemistry Letters（2017）

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摘要

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.

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关键词

Kynurenine,Monooxygenase,Tryptophan,Substrate,Pancreatitis

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