1750-47-6Relevant academic research and scientific papers
Development of a Series of Kynurenine 3-Monooxygenase Inhibitors Leading to a Clinical Candidate for the Treatment of Acute Pancreatitis
Walker, Ann L.,Ancellin, Nicolas,Beaufils, Benjamin,Bergeal, Marylise,Binnie, Margaret,Bouillot, Anne,Clapham, David,Denis, Alexis,Haslam, Carl P.,Holmes, Duncan S.,Hutchinson, Jonathan P.,Liddle, John,McBride, Andrew,Mirguet, Olivier,Mowat, Christopher G.,Rowland, Paul,Tiberghien, Nathalie,Trottet, Lionel,Uings, Iain,Webster, Scott P.,Zheng, Xiaozhong,Mole, Damian J.
, p. 3383 - 3404 (2017)
Recently, we reported a novel role for KMO in the pathogenesis of acute pancreatitis (AP). A number of inhibitors of kynurenine 3-monooxygenase (KMO) have previously been described as potential treatments for neurodegenerative conditions and particularly for Huntington’s disease. However, the inhibitors reported to date have insufficient aqueous solubility relative to their cellular potency to be compatible with the intravenous (iv) dosing route required in AP. We have identified and optimized a novel series of high affinity KMO inhibitors with favorable physicochemical properties. The leading example is exquisitely selective, has low clearance in two species, prevents lung and kidney damage in a rat model of acute pancreatitis, and is progressing into preclinical development.
Allelopathic potential of 5-chloro-6-methoxy-2-benzoxazolinone
Kato-Noguchi, Hisashi,Kosemura, Seiji,Yamamura, Shosuke
, p. 433 - 435 (1998)
A new benzoxazolinone, 5-chloro-6-methoxy-2-benzoxazolinone (Cl-MBOA) caused growth inhibition of roots and shoots of oat (Avena sativa), timothy (Phleum pratense), crabgrass (Digitaria sanguinalis), ryegrass (Lolium multiflorum), cockscomb (Amaranthus caudatus), cress (Lepidium sativum) and lettuce (Lactuca sativa); increasing the dose of Cl-MBOA increased inhibition. The concentrations for 40% inhibition of root growth were 0.12, 0.14, 0.17, 0.19, 0.46, 0.57 and 0.76 mM for timothy, crabgrass, ryegrass, oat, cockscomb, cress and lettuce, respectively, and the concentrations for 40% inhibition of shoot growth were 0.25, 0.28, 0.36, 0.40, 7.9, 12.5 and 19.6 mM for timothy, crabgrass, ryegrass, cockscomb, cress and lettuce, respectively. The contents of Cl-MBOA in shoots and roots of 14-day-old maize (Zea mays) seedlings were 37.5 and 8.7 μg g-1 fr. wt. The presence of this compound in maize seedlings, coupled with its effect on growth, suggest that it may play an important role in maize allelopathy.
