Abstract
Abstract (E)-N’-Benzylidene-7-methyl-2-propyl-1H-benzo [d]imidazole-5-carbohydrazides (5a-r) have been synthesized from 7-methyl-2-propyl-1H-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.
Highlights
Non-steroidal anti-inflammatory drugs (NSAIDs) are considered as one of the most widely used therapeutics to5-Substituted benzimidazoles are privileged heterocycles for medicinal chemists due to their broad range of biological activities such as anti-inflammatory [3], anticancer [4] and benimidazole-5-carboxylic acid and its derivatives are promising agents for hepatitis C virus infections [5, 6, 7], Glycoprotein IIb/ IIIa inhibitors [8], Glutaminyl Cyclase inhibitors [9], and checkpoint kinase inhibitor [10] activities
Based on the pharmacological activities of both the benzimidazoles and hydrazones, and our quest in search of new biologically active molecules [22,23,24], we report the design, synthesis, antioxidant, anti-inflammatory and analgesic activity of (E)-N’-Benzylidene-7-methyl-2-propyl1H-benzo[d]imidazole-5-carbohydrazides (5a-r)
Compound-1 was reduced with Na2S2O4 in water to afford methyl 3-amino-4-butyriamido-4-methylbenzoate, which in turn internally cyclised by nucleophilic addition of amino group to the adjacent amide carbonyl to form compound-2
Summary
Abstract: (E)-N’-Benzylidene-7-methyl-2-propyl-1H-benzo [d]imidazole-5-carbohydrazides (5a-r) have been synthesized from 7-methyl-2-propyl-1H-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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