One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, category: Thiomorpholine, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 39093-93-1, Name is Thiomorpholine 1,1-dioxide, molecular formula is C4H9NO2S
Morpholylureas are a new class of potent and selective inhibitors of the type 5 17-beta-hydroxysteroid dehydrogenase (AKR1C3)
Inhibitors of the aldo-keto reductase enzyme AKR1C3 are of interest as potential drugs for leukemia and hormone-related cancers A series of non-carboxylate morpholino(phenylpiperazin-1-yl)methanones were prepared by palladium-catalysed coupling of substituted phenyl or pyridyl bromides with the known morpholino(piperazin-1-yl)methanone, and shown to be potent (IC 50 ? 100 nM) and very isoform-selective inhibitors of AKR1C3 Lipophilic electron-withdrawing substituents on the phenyl ring were positive for activity, as was an H-bond acceptor on the other terminal ring, and the ketone moiety (as a urea) was essential These structure-activity relationships are consistent with an X-ray structure of a representative compound bound in the AKR1C3 active site, which showed H-bonding between the carbonyl oxygen of the drug and Tyr55 and His117 in the ‘oxyanion hole’ of the enzyme, with the piperazine bridging unit providing the correct twist to allow the terminal benzene ring to occupy the lipophilic pocket and align with Phe311
Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.category: Thiomorpholine, you can also check out more blogs about39093-93-1
Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem