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-  2018 

Impact of novel N

DOI: 10.1177/1753425917740727

Keywords: Nitric oxide,Alzheimer’s disease,N-aryl piperamides,cyclooxygenase type 2,ADMET,docking

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Abstract:

NO donor drugs showed a significant therapeutic effect in the treatment of many diseases, such as arteriopathies, various acute and chronic inflammatory conditions, and several degenerative diseases. NO-releasing anti-inflammatory drugs are the prototypes of a novel class of compounds, combining the pharmacological activities of anti-inflammatory and anti-nociceptive of drugs with those of NO, thus possessing potential therapeutic applications in a great variety of diseases. In this study, we designed and predicted biological activity by targeting cyclooxygenase type 2 (COX-2) and NF-κB subunits and pharmacological profiling along with toxicity predictions of various N-aryl piperamides linked via an ester bond to a spacer that is bound to a NO-releasing moiety (-ONO2). The result of absorption, distribution, metabolism and excretion and Docking studies indicated that among 51 designed molecules PA-3′K showed the best binding potential in both the substrate and inhibitory binding pocket of the COX-2 enzyme with affinity values of –9.33 and –5.12 for PDB ID 1CVU and 3LN1, respectively, thereby having the potential to be developed as a therapeutic agent. The results of cell viabilities indicated that PA-3′k possesses the best cell viability property with respect to its dose (17.33?ng/ml), with 67.76% and 67.93% viable cells for CHME3 and SVG cell lines, respectively

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