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
GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.
GlaxoSmithKline, Les Ulis, Paris, France.
Bioorg Med Chem Lett. 2017 May 1;27(9):2023-2028. doi: 10.1016/j.bmcl.2017.02.078. Epub 2017 Mar 9.
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.
通过基于底物的方法发现了一系列用于治疗急性胰腺炎的强效、竞争性且高度选择性的犬尿氨酸单加氧酶抑制剂。先导化合物在体内表现出良好的细胞活性和明确的药效学活性。
