Department Of Pharmacology

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Browsing Department Of Pharmacology by Author "Aggarwal, Ranjana"

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    Design, synthesis, and biological evaluation of N-[1-(6?-chloropyridazin-3?-yl)-3-(4?-substitutedphenyl)-1H-pyrazole-5-yl]alkanamides as anti-inflammatory agents
    (John Wiley and Sons Inc, 2022-01-22T00:00:00) Aggarwal, Ranjana; Swati, S.; Kumar, Vinod; Singh, Randhir; Kajal, Anu; Saini, Deepika
    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. � 2022 Wiley Periodicals LLC.