Roever, Stephan; Cesura, Andrea M.; Huguenin, Philipp; Kettler, Rolf; Szente, Andre published the artcile< Synthesis and Biochemical Evaluation of N-(4-Phenylthiazol-2-yl)benzenesulfonamides as High-Affinity Inhibitors of Kynurenine 3-Hydroxylase>, Quality Control of 57493-24-0, the main research area is phenylthiazolylbenzensulfonamide preparation kynurenine hydroxylase inhibitor; thiazolylbenzensulfonamide preparation kynurenine hydroxylase inhibitor; structure activity phenylthiazolylbenzenesulfonamide kynurenine hydroxylase inhibitor.
The synthesis, structure-activity relationship (SAR), and biochem. characterization of N-(4-phenylthiazol-2-yl)benzenesulfonamides as inhibitors of kynurenine 3-hydroxylase is described. Thiazolbenzenesulfonamides I (IC50 = 37 nM, Ro-61-8048) and and II (IC50 = 19 nM) were high-affinity inhibitors of this enzyme in vitro. In addition, both compounds blocked rat and gerbil kynurenine 3-hydroxylase after oral administration, with ED50’s in the 3-5 μmol/kg range in gerbil brain. In a microdialysis experiment in rats, I dose dependently increased kynurenic acid concentration in the extracellular hippocampal fluid. A dose of 100 μmol/kg po led to a 7.5-fold increase in kynurenic acid outflow. These new compounds should allow detailed investigation of the pathophysiol. role of the kynurenine pathway after neuronal injury.
Journal of Medicinal Chemistry published new progress about Structure-activity relationship, enzyme-inhibiting. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Quality Control of 57493-24-0.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica