Journal of Pharmaceutics & Drug Delivery ResearchISSN: 2325-9604

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Effect of novel nitric oxide donor N-aryl piperamide derivatives on neuroinflammation and degeneration diseases and the prediction of ADMET profiles


Sajad Shahbazi and Ranbir Chander Sobti

Panjab University, India
Babasaheb Bhimrao Ambedkar University, India

: J Pharm Drug Deliv Res

Abstract


Through discovery of the various pathophysiological and physiological processes involving nitric oxide (NO), the most attempts were focused on developing new drugs with capability to modulate NO production directly and/or indirectly for therapeutic purposes such as NO-releasing drugs, NO-inhibiting drugs, and phosphodiesterase V inhibitors. NO donor drugs showed an important therapeutic effect in the treatment of many diseases such as arteriopathies, various acute and chronic inflammatory conditions, and several degenerative diseases (Alzheimer’s disease and cancer). Nitric oxide (NO)-releasing anti-inflammatory drugs are the prototypes of novel class of compounds that, combining the pharmacological activities of anti-inflammatory and antinociceptive of drugs with those of NO (vasodilator, anti-aggregant, antimicrobial and immune modulator agent), possess potential therapeutic applications in a great variety of diseases. The anti-inflammatory activity of different N-Aryl Piperamides (NAP) have been screened and verified in our previous study and different other reports. In this study, we designed and predicted the biological activity by targeting cyclooxygenase type 2 and pharmacological profiling along with toxicity predictions of various NAPs linked via an ester bond to a spacer that is bound to a Nitric Oxide (NO)- releasing moiety (-ONO2). The result of ADMET and Docking study indicated that among 44 designed molecules, 2-((2E,4E)- 5-(benzo[d][1,3]dioxol-5-yl)-N-(4-(1-hydroxyethyl) phenyl)penta-2,4-dienamido) ethyl nitrate with code number 2e showed the best binding potential in both substrate and inhibitory binding pocket of COX-2 enzyme with affinity values -9.33 and -5.12 for PDB ID:1CVU and 3LN1 respectively, thereby, having the potential to be developed as therapeutic agent.

Biography


Email: sajad642008@gmail.com

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