The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 27492-84-8, Name is Methyl 4-amino-2-methoxybenzoate, SMILES is O=C(OC)C1=CC=C(N)C=C1OC, in an article , author is Nija, B., once mentioned of 27492-84-8, Safety of Methyl 4-amino-2-methoxybenzoate.
Development, Characterization, and Pharmacological Investigation of Sesamol and Thymol Conjugates of Mefenamic Acid
BACKGROUND Prodrug technology was extensively employed in the drug discovery processes and many approved drugs in the pharmaceutical industry were developed by the prodrug based synthetic approach. The current research work investigates the effect of the prodrug approach on the mefenamic acid by synthesizing the ester conjugates with natural antioxidants such as sesamol and thymol. METHODS Synthesis of two ester prod rugs, mefenamic acid-sesamol conjugate and mefenamic acid-thymol conjugate by coupling method using DCC / DMAP, subjected to physicalchemical characterization, spectral characterization (IR, H-1 NMR, C-13 NMR and Mass spectra), in-silico studies, in-vivo biodistribution studies and pharmacological evaluation such as anti-inflammatory, ulcerogenecity, activity in the brain as well as histopathological evaluation. RESULTS The ester prodrugs of mefenamic acid which upon administration would release the parent drug as a result of enzymatic or non-enzymatic hydrolysis in the desired areas with enhanced anti-inflammatory activity and reduction in the gastro intestinal toxicity. In-silico studies showed the docking score of mefenamic acid on the beta-secretase enzyme is – 7.834 and the bio-distribution study showed the enhanced distribution of the mefenamic acid in the brain. Pharmacological study and histopathology studies using the brain tissues showed the protective effect of mefenamic acid in the brain. CONCLUSIONS Antioxidant conjugates of mefenamic acid showed sustained release of the mefenamic acid and enhanced anti-inflammatory activity with reduction in the gastric toxicity. The present investigation also revealed that the enhanced transport profile across blood brain barrier and considerable protective effect in the brain against neurodegenerative conditions.
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