R. Aggarwal, Swati , Vinod Kumar
May 1, 2022
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Journal
Drug Development Research
Abstract
A series of structurally diverse N‐[1‐(6′‐chloropyridazin‐3′‐yl)‐3‐(4″‐substitutedphenyl)‐1H‐pyrazole‐5‐yl]alkanamides 5(a–r) has been designed and synthesized via Aliquat 336 catalyzed amidation of 5‐amino‐3‐aryl‐1‐(6′‐chloropyridazin‐3′‐yl)pyrazoles 3(a–c). The target compounds were designed on basis of the results obtained from the study of Lipinski's rule of five and binding interactions with target protein 3LN1. Eventually, compounds 5(a–r) were screened for their in vitro anti‐inflammatory action by using inhibition of albumin denaturation and membrane stabilization assay. It has been found that all the synthesized compounds obeyed Lipinski's rule of five (nviolations = 0–1) and showed weak to strong binding interactions with dock score range −8.0 to −9.9 kcal/mol. All alkanamides exhibited moderate to excellent activity as compared to the standard drug, Aspirin. Interestingly, the results indicated that the compound 5a may act as a promising medicinal lead as an anti‐inflammatory agent for in vivo and clinical testing in future.