One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Application In Synthesis of 6-Bromo-1,2,3,4-tetrahydroisoquinoline, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 226942-29-6, Name is 6-Bromo-1,2,3,4-tetrahydroisoquinoline, molecular formula is C9H10BrN
3-(3,4-dihydroisoquinolin-2(1 H)-ylsulfonyl)benzoic acids: Highly potent and selective inhibitors of the type 5 17-beta-hydroxysteroid dehydrogenase AKR1C3
A high-throughput screen identified 3-(3,4-dihydroisoquinolin-2(1H)- ylsulfonyl)benzoic acid as a novel, highly potent (low nM), and isoform-selective (1500-fold) inhibitor of aldo-keto reductase AKR1C3: a target of interest in both breast and prostate cancer. Crystal structure studies showed that the carboxylate group occupies the oxyanion hole in the enzyme, while the sulfonamide provides the correct twist to allow the dihydroisoquinoline to bind in an adjacent hydrophobic pocket. SAR studies around this lead showed that the positioning of the carboxylate was critical, although it could be substituted by acid isosteres and amides. Small substituents on the dihydroisoquinoline gave improvements in potency. A set of “reverse sulfonamides” showed a 12-fold preference for the R stereoisomer. The compounds showed good cellular potency, as measured by inhibition of AKR1C3 metabolism of a known dinitrobenzamide substrate, with a broad rank order between enzymic and cellular activity, but amide analogues were more effective than predicted by the cellular assay.
One of the oldest and most widely used commercial enzyme inhibitors is aspirin, Application In Synthesis of 6-Bromo-1,2,3,4-tetrahydroisoquinoline, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 226942-29-6
Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem