Heterocyclic Communications · 2019 · 23 citations · 26 references
PharmacyMedicinal ChemistryPharmacologyDrug DiscoveryMolecular PharmacologyStructure-activity RelationshipsAnalgesic PharmacologyAnti-inflammatory PharmacologyStructure-activity Relationship AnalysisAldehydesAnalgesic Anti-inflammatory PharmacologyAntioxidant Activity AssaysAntioxidant PropertiesBiological Evaluation ReportDocking StudiesImidazole ChemistryMolecular Docking Analysis
Abstract ( E )- N ’-Benzylidene-7-methyl-2-propyl-1 H -benzo [ d ]imidazole-5-carbohydrazides (5a-r) have been synthesized from 7-methyl-2-propyl-1 H -benzo[ d ]imidazole-5-carbohydrazide ( 3 ) by condensing with different aromatic aldehydes ( 4a-r ). Title compounds ( 5a-r ) were evaluated for in vitro antioxidant activity and based on their potential for antioxidant property, selected compounds 5d and 5m-p were screened for in vivo anti-inflammatory and analgesic activity. The results indicate that the compound 5o and 5p are effective against anti-inflammatory and analgesic activity. The biological data was further supported by molecular docking studies, which revealed the binding pattern and the affinity of the molecules in the active site of COX-2.
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Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents
Ravi G. Kurumbail, Anna M. Stevens, James K. Gierse et al. · Nature · 1996 · 1.9K citations