Can You Really Do Chemisty Experiments About 96-53-7

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 96-53-7. HPLC of Formula: C3H5NS2.

Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 96-53-7, Name is 4,5-Dihydrothiazole-2-thiol, molecular formula is C3H5NS2, belongs to thiazoles compound. In a document, author is Barnette, Dustyn A., introduce the new discover, HPLC of Formula: C3H5NS2.

Meloxicam methyl group determines enzyme specificity for thiazole bioactivation compared to sudoxicam

Meloxicam is a thiazole-containing NSAID that was approved for marketing with favorable clinical outcomes despite being structurally similar to the hepatotoxic sudoxicam. Introduction of a single methyl group on the thiazole results in an overall lower toxic risk, yet the group’s impact on P450 isozyme bioactivation is unclear. Through analytical methods, we used inhibitor phenotyping and recombinant P450s to identify contributing P450s, and then measured steady-state kinetics for bioactivation of sudoxicam and meloxicam by the recombinant P450s to determine relative efficiencies. Experiments showed that CYP2C8, 2C19, and 3A4 catalyze sudoxicam bioactivation, and CYP1A2 catalyzes meloxicam bioactivation, indicating that the methyl group not only impacts enzyme affinity for the drugs, but also alters which isozymes catalyze the metabolic pathways. Scaling of relative P450 efficiencies based on average liver concentration revealed that CYP2C8 dominates the sudoxicam bioactivation pathway and CYP2C9 dominates meloxicam detoxification. Dominant P450s were applied for an informatics assessment of electronic health records to identify potential correlations between meloxicam drug-drug interactions and drug-induced liver injury. Overall, our findings provide a cautionary tale on assumed impacts of even simple structural modifications on drug bioactivation while also revealing specific targets for clinical investigations of predictive factors that determine meloxicam-induced idiosyncratic liver injury. (C) 2020 Elsevier B.V. All rights reserved.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 96-53-7. HPLC of Formula: C3H5NS2.

Reference:
Thiazole | C3H3NS – PubChem,
,Thiazole | chemical compound | Britannica