[Synthesis and antiinflammatory activity of 2-(E)-(4-hydroxy-3-methoxybenzylidene)-5-(N-substituted aminomethyl)
Abstract:
In search for new antiinflammatory agents, a series of 2-(E)-(4-hydroxy-3-methoxybenzylidene)-5-(N-substituted aminomethyl) cyclopentanones was synthesized via Stork reaction, Mannich reaction and amine exchange reaction. All of the fifteen target compounds were characterized by spectral analysis and elemental analysis. Preliminary pharmacological tests showed that several target compounds exerted appreciable effect on xylene-induced ear edema in mice and that alteration of the substituents of anilines showed significant influence on antiinflammatory potency.
More Related Videos
07:36Analysis of Raw and Processed Cyperi Rhizoma Samples Using Liquid Chromatography-Tandem Mass Spectrometry in Rats with Primary Dysmenorrhea
Published on: December 23, 2022
11:04Preparation of Enantiopure Non-Activated Aziridines and Synthesis of Biemamide B, D, and epiallo-Isomuscarine
Published on: June 13, 2022
Related Concept Videos
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of the aromatic...
Adrenergic Agonists: Mixed-Action Agents
Ephedrine and pseudoephedrine lack a catecholamine group, making them less susceptible to degradation by metabolic enzymes. They have increased oral bioavailability and lipophilicity, resulting in a longer duration of action. Their response is reduced by...
Aromatic Hydrocarbon Anions: Structural Overview
Due to the absence of continuous overlap of p...
Stability of Substituted Cyclohexanes
The two chair conformations of cyclohexanes undergo rapid interconversion at room temperature. Both forms have identical energies and stabilities, each comprising equal amounts of the equilibrium mixture. Replacing a hydrogen atom with a functional group makes the two conformations energetically non-equivalent.
For example, in...
ortho–para-Directing Activators: –CH3, –OH, –⁠NH2, –OCH3
Preparation of Epoxides
Epoxides result from alkene oxidation, which can be achieved by a) air, b) peroxy acids, c) hypochlorous acids, and d) halohydrin cyclization.
Epoxidation with Peroxy Acids
Epoxidation of alkenes via oxidation with peroxy acids involves the conversion of a carbon–carbon double bond to an epoxide using the oxidizing agent meta-chloroperoxybenzoic acid, commonly known as MCPBA. Since the O–O bond of peroxy acids is very weak, the addition of electrophilic oxygen of peroxy acids to...
