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

John Liddle; Benjamin Beaufils; Margaret Binnie; Anne Bouillot; Alexis A Denis; Michael M Hann; Carl P 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 J Uings; Ann L Walker; Scott P Webster

doi:10.1016/j.bmcl.2017.02.078

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

John Liddle, Benjamin Beaufils, Margaret Binnie, Anne Bouillot, Alexis A Denis, Michael M Hann, Carl P 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 J Uings, Ann L Walker, Scott P Webster

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Abstract / Description of output

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.

Original language	English
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	27
Issue number	9
Early online date	9 Mar 2017
DOIs	https://doi.org/10.1016/j.bmcl.2017.02.078
Publication status	Published - May 2017

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Journal Article

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10.1016/j.bmcl.2017.02.078

Discovery of KMO Inhibitors BMCL Feb 27 2017
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Accepted author manuscript, 1.26 MB

Chris Mowat
- School of Chemistry - Senior Lecturer
- EaStCHEM
Person: Academic: Research Active

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Liddle, J., Beaufils, B., Binnie, M., Bouillot, A., Denis, A. A., Hann, M. M., Haslam, C. P., Holmes, D. S., Hutchinson, J. P., Kranz, M., McBride, A., Mirguet, O., Mole, D. J., Mowat, C. G., Pal, S., Rowland, P., Trottet, L., Uings, I. J., Walker, A. L., & Webster, S. P. (2017). The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis. Bioorganic & Medicinal Chemistry Letters, 27(9). https://doi.org/10.1016/j.bmcl.2017.02.078

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

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.",

keywords = "Journal Article",

author = "John Liddle and Benjamin Beaufils and Margaret Binnie and Anne Bouillot and Denis, {Alexis A} and Hann, {Michael M} and Haslam, {Carl P} and Holmes, {Duncan S} and Hutchinson, {Jon P} and Michael Kranz and Andrew McBride and Olivier Mirguet and Mole, {Damian J} and Mowat, {Christopher G} and Sandeep Pal and Paul Rowland and Lionel Trottet and Uings, {Iain J} and Walker, {Ann L} and Webster, {Scott P}",

note = "Copyright {\textcopyright} 2017. Published by Elsevier Ltd.",

year = "2017",

month = may,

doi = "10.1016/j.bmcl.2017.02.078",

language = "English",

volume = "27",

journal = "Bioorganic & Medicinal Chemistry Letters",

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Liddle, J, Beaufils, B, Binnie, M, Bouillot, A, Denis, AA, Hann, MM, Haslam, CP, Holmes, DS, Hutchinson, JP, Kranz, M, McBride, A, Mirguet, O, Mole, DJ , Mowat, CG, Pal, S, Rowland, P, Trottet, L, Uings, IJ, Walker, AL & Webster, SP 2017, 'The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis', Bioorganic & Medicinal Chemistry Letters, vol. 27, no. 9. https://doi.org/10.1016/j.bmcl.2017.02.078

TY - JOUR

T1 - The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis

AU - Liddle, John

AU - Beaufils, Benjamin

AU - Binnie, Margaret

AU - Bouillot, Anne

AU - Denis, Alexis A

AU - Hann, Michael M

AU - Haslam, Carl P

AU - Holmes, Duncan S

AU - Hutchinson, Jon P

AU - Kranz, Michael

AU - McBride, Andrew

AU - Mirguet, Olivier

AU - Mole, Damian J

AU - Mowat, Christopher G

AU - Pal, Sandeep

AU - Rowland, Paul

AU - Trottet, Lionel

AU - Uings, Iain J

AU - Walker, Ann L

AU - Webster, Scott P

PY - 2017/5

Y1 - 2017/5

N2 - 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.

AB - 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.

KW - Journal Article

U2 - 10.1016/j.bmcl.2017.02.078

DO - 10.1016/j.bmcl.2017.02.078

M3 - Article

C2 - 28336141

SN - 0960-894X

VL - 27

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 9

ER -

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

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Chris Mowat

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