20532-28-9, Chemical Research Letters, May 2021. The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. In a article, 20532-28-9, molcular formula is C8H7NS, introducing its new discovery.
A novel series of potent and selective non-peptide neuropeptide Y (NPY) Y1 receptor antagonists, having benzazepine nuclei, have been designed, synthesized, and evaluated for activity. Chemical modification of the R1 and R3 substituents in structure 1 (Chart 1) yields several compounds that show high affinity for the Y1 receptor (K(i) values of less than 10 nM). SAR studies revealed that introduction of an isopropylurea group at R1 and a 3- (benzo-condensed-urea) group, 3-(fluorophenylurea) group, or a 3-(N-(4- hydroxyphenyl)guanidine) group at R3 in structure 1 afforded potent and subtype-selective NPY Y1 receptor antagonists. 3-(3-(Benzothiazol-6- yl)ureido)-1-N-(3-(N’-(3-isopropylureido))benzyl)-2,3,4,5-tetrahydro-1H-1- benzazepin-2-one (21), which was one of the most potent derivatives, competitively inhibited specific [125I]peptide YY (PYY) binding to Y1 receptors in human neuroblastoma SK-N-MC cells (K(i) = 5.1 nM). 21 not only inhibited the Y1 receptor-mediated increase in cytosolic free Ca2+ concentration in SK-N-MC cells but also antagonized the Y1 receptor-mediated inhibitory effect of peptide YY on gastrin-induced histamine release in rat enterochromaffin-like cells. 21 showed no significant affinity in 17 receptor binding assays including Y2, Y4, and Y5 receptors.
Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. 20532-28-9, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 20532-28-9, in my other articles.
Reference：
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem