The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 4-Hydroxyquinoline-2-carboxylic Acid(SMILESS: O=C(C1=NC2=CC=CC=C2C(O)=C1)O,cas:492-27-3) is researched.Application In Synthesis of 5-Methylfuran-2(3H)-one. The article 《Assessment of the safety, pharmacokinetics and pharmacodynamics of GSK3335065, an inhibitor of kynurenine monooxygenase, in a randomized placebo-controlled first-in-human study in healthy volunteers》 in relation to this compound, is published in British Journal of Clinical Pharmacology. Let’s take a look at the latest research on this compound (cas:492-27-3).
GSK3335065 is an inhibitor of kynurenine monooxygenase (KMO) being developed for the treatment of acute pancreatitis. Healthy male volunteers were administered ascending doses of GSK3335065 or matched placebo as a single i.v. bolus injection to assess safety, tolerability, pharmacokinetics and pharmacodynamics. GSK3335065 displayed an apparent volume of distribution between 20.6 L and 44.6 L, a clearance between 0.462 L/h and 0.805 L/h and a terminal half-life between 31.3 and 34.5 h. In the single subject who received 1.3 mg GSK3335065, changes in tryptophan pathway metabolites were observed consistent with the changes seen in preclin. species suggesting that KMO enzyme activity was partially inhibited. However, a broad complex ventricular tachycardia was observed in this subject, which was judged to be a Serious Adverse Event (SAE) and resulted in early termination of the study. While development of GSK3335065 was subsequently discontinued, significant confounding factors hinder a clear interpretation that the tachycardia was directly related to administration of the compound
Compound(492-27-3)HPLC of Formula: 492-27-3 received a lot of attention, and I have introduced some compounds in other articles, similar to this compound(4-Hydroxyquinoline-2-carboxylic Acid), if you are interested, you can check out my other related articles.
Reference:
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”