Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In an article, author is Kaur, Sukhmeet, once mentioned the application of 41979-39-9, Name is Piperidin-4-one hydrochloride, molecular formula is C5H10ClNO, molecular weight is 135.592, MDL number is MFCD00041019, category is piperidines. Now introduce a scientific discovery about this category, Safety of Piperidin-4-one hydrochloride.
Design and Synthesis of Aza-/Oxa Heterocycle-Based Conjugates as Novel Anti-Inflammatory Agents Targeting Cyclooxygenase-2
A library of hybrid molecules was procured by the combination of triazine-indole adduct with morpholine/ piperidine/pyrrolidine and pyrazole/pyrimidine/oxindole moieties. Enzyme immunoassays on cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) identified compound 6 having an IC50 value of 20 nM for COX-2 and 3000 nM for COX-1. The significant reduction in the formation of prostaglandin E-2 in the lipopolysaccharide-treated (COX-2-activated) human whole blood, almost no change in the production of thromboxane B-2 in the calcium ionophore-treated (COX-1-activated) sample of human whole blood, and the mechanistic studies on Swiss albino mice ensured that compound 6 is selective for COX-2. The association constant (K-a) of compound 6 with COX-2 was found to be of the order of 0.48 x 10(6) M-1. The diffusion spectroscopy experiments and relaxation time (T-1) calculations of compound 6 in the presence of COX-2 assisted in identifying the site-specific interactions of 6 with the enzyme, and these results fall into nice correlation with the theoretical data obtained from molecular docking and quantitative structure-activity relationship studies. With maximum tolerable dose >2000 mg kg(-1), compound 6 made 68 and 32% reduction in formalin-induced analgesia and carrageenan-induced inflammation in Swiss albino mice.
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Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem