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A selective method was developed for the synthesis of acyclic sulfanyl derivatives of ampyrone by thiomethylation reaction of 4-amino- 2,3-dimethyl-1-phenyl-3-pyrazolin-5-one with formaldehyde and thiols in aqueous medium under various conditions… Click to show full abstract
A selective method was developed for the synthesis of acyclic sulfanyl derivatives of ampyrone by thiomethylation reaction of 4-amino- 2,3-dimethyl-1-phenyl-3-pyrazolin-5-one with formaldehyde and thiols in aqueous medium under various conditions (room temperature, 80°C, ultrasonication or microwave irradiation). A series of the synthesized sulfanyl derivatives of ampyrone were characterized with regard to their anti-inflammatory activity by molecular docking method using the AutoDock 4.2 and AutoDock Vina software. The steric complementarity with the active sites of cyclooxygenase isoforms (COX-1 and COX-2) was explored.
Journal Title: Chemistry of Heterocyclic Compounds
Year Published: 2020
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