Research speed reading in 2021. Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent,Which mentioned a new discovery about Electric Literature of 42923-79-5, molcular formula is C9H10N2O2, introducing its new discovery. , Electric Literature of 42923-79-5
7-(Aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK and F 29661, 1) is a potent inhibitor of the enzyme phenylethanolamine N-methyltransferase (PNMT, EC 2.1.1.28). In contrast to other inhibitors of PNMT, it is also highly selective toward PNMT in comparison with its affinity toward the alpha2- adrenoceptor (PNMT K(i) = 0.55 muM, alpha2 K(i) = 100 muM, selectivity [alpha2 K(i)/PNMT K(i)] = 180). A diverse set of compounds was synthesized and evaluated to probe the role of the acidic hydrogen of the aminosulfonyl group of 1 in imparting this selectivity. Compounds were designed to investigate the effect on selectivity of the acidity of the NH group [the 7-N-methyl (compound 5) and 7-N-(p-chlorophenyl) (compound 4) derivatives of 1], the relative spatial position of the acidic hydrogen [7-(N- (methylsulfonyl)amino)-1,2,3,4-tetrahydroisoquinoline (6) and 7-((N- (methylsulfonyl)amino)methyl)-1,2,3,4-tetrahydroisoquinoline (8)], or the effect of the substitution of an acidic phenolic group for the aminosulfonyl moiety [1-(aminomethyl)-6-hydroxynaphthalene (28) and 8-hydroxy-1,2,3,4- tetrahydrobenz[h]isoquinoline (9)]. All of the compounds studied displayed lower affinity for PNMT than 1, and nine of the eleven compounds studied showed increased, rather than the desired decreased, affinity for the alpha2- adrenoceptor. Specifically, compound 4, in which the aminosulfonyl NH group is more acidic than that in 1, showed greatly reduced selectivity on account of increased alpha2-adrenoceptor affinity as compared to 1 (PNMT K(i) =- 2.6 muM, alpha2 K(i) = 6.3 muM, selectivity = 2.4). Compound 8, in which the acidic NH group is in the same region of space as that in 1, although the aminosulfonyl group is reversed with respect to the aromatic ring, showed poor PNMT affinity and modest alpha2-adrenoceptor affinity (PNMT K(i) = 330 muM, alpha2 K(i) = 18 muM, selectivity = 0.055). Compound 9, in which a phenolic group is in the same region of space as the acidic NH of 1, exhibited the best alpha2-adrenoceptor affinity of any of the compounds studied (PNMT K(i) = 0.98 muM, alpha2 K(i) = 0.078 muM, selectivity = 0.080). Results from this study suggest that the selectivity of 1 is not solely due to the presence of an acidic hydrogen on the 7-aminosulfonyl group of 1 but is likely also dependent on some other property (e.g. electron-withdrawing character) of the aminosulfonyl group.
The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 42923-79-5 is helpful to your research. Electric Literature of 42923-79-5
Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem