Reference of 824-79-3, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 824-79-3, Name is Sodium 4-methylbenzenesulfinate, SMILES is O=S(C1=CC=C(C)C=C1)[O-].[Na+], belongs to isothiazole compound. In a article, author is Perrone, Maria Grazia, introduce new discover of the category.
Diarylheterocycle Core Ring Features Effect in Selective COX-1 Inhibition
The COX-1 isoenzyme plays a significant role in a variety of diseases, as it catalyzes the bioprocesses behind many health problems. Among the diarylheterocycle class of COX inhibitors, the isoxazole ring has been widely used as a central heterocycle for the preparation of potent and selective COX-1 inhibitors such as P6 [3-(5-chlorofuran-2-yl)-5-methyl-4-phenylisoxazole]. The role of the isoxazole nucleus in COX-1 inhibitor selectivity has been clarified by preparing a set of new diarylheterocycles with various heterocycle cores. Replacement of isoxazole with isothiazole or pyrazole gave a drastic decrease in COX-1 inhibitory activity, whereas the introduction of an electron-donating group (EDG) on the N-aryl pyrazole allowed recovery of COX-1 inhibitory activity and selectivity. The EDG-equipped 5-(furan-2-yl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazole (17) selectively inhibits COX-1 activity (IC50=3.4 mu M; 28?% COX-2 inhibition at 50 mu M), in contrast to its inactive analogue, 3-(furan-2-yl)-1-phenyl-5-(trifluoromethyl)-1H-pyrazole, which does not bear the methoxy EDG. Molecular docking studies of compound 17 into the binding site of COX-1 shed light on its binding mode.
Reference of 824-79-3, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 824-79-3.
Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com