One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Quality Control of [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium(II), such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 72287-26-4, Name is [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium(II), molecular formula is C34H28Cl2FeP2Pd
Development of alpha-glucosidase inhibitors by room temperature C-C cross couplings of quinazolinones
Novel quinazolinone based alpha-glucosidase inhibitors have been developed. For this purpose a virtual screening model has been generated and validated utilizing acarbose as a alpha-glucosidase inhibitor. Homology modeling, docking, and virtual screening were successfully employed to discover a set of structurally diverse compounds active against alpha-glucosidase. A search of a 3D database containing 22 500 small molecules using the structure based virtual model yielded ten possible candidates. All ten candidates were N-3-pyridyl-2-cyclopropyl quinazolinone-4-one derivatives, varying at the 6 position. This position was modified by Suzuki-Miyaura cross coupling with aryl, heteroaryl, and alkyl boronic acids. A catalyst screen was performed, and using the best optimal conditions, a series of twenty five compounds was synthesized. Notably, the C-C cross coupling reactions of the 6-bromo-2-cyclopropyl-3- (pyridyl-3-ylmethyl)quinazolin-4(3H)-one precursor have been accomplished at room temperature. A comparison of the relative reactivities of 6-bromo and 6-chloro-2,3-disubstituted quinazolinones with phenyl boronic acid was conducted. An investigation of pre-catalyst loading for the reaction of the 6-bromo-2-cyclopropyl-3-(pyridyl-3-ylmethyl)quinazolin-4(3H)-one substrate was also carried out. Finally, we submitted our compounds to biological assays against alpha-glucosidase inhibitors. Of these, three hits (compounds 4a, 4t and 4r) were potentially active as alpha-glucosidase inhibitors and showed activity with IC50 values <20 muM. Based on structural novelty and desirable drug-like properties, 4a was selected for structure-activity relationship study, and thirteen analogs were synthesized. Nine out of thirteen analogs acted as alpha-glucosidase inhibitors with IC50 values <10 muM. These lead compounds have desirable physicochemical properties and are excellent candidates for further optimization. One of the oldest and most widely used commercial enzyme inhibitors is aspirin, Quality Control of [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium(II), which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 72287-26-4
Reference£º
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method