Synthesis and Pharmacological Evaluation of Novel 1-(2-(Benzoyl-Substituted-2-phenyl-1H-Indol-5-Carbony) Hydrazinyloxy) Vinyl Nitrate Derivatives as Potent Non-Ulcerogenic, Analgesic and Anti-Inflammatory Agents

Author(s): Vinod J. Mokale, Mayuresh K. Raut, Prashant J. Burange, Navneet S. Dhoot, Shashikant V. Bhandari, Kailash G. Bothara, Jitendra B. Naik.

Journal Name: Medicinal Chemistry

Volume 6 , Issue 4 , 2010

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Abstract:

Six derivatives of 1-(2-(benzoyl-(substituted)-2-phenyl-1H-indole-5-carbony) hydrazinyloxy) vinyl nitrate were synthesized and tested in vivo for anti-inflammatory, analgesic, and ulcerogenic properties. Synthesized compounds shown significant anti-inflammatory activity comparable to that of Diclofenac sodium in the carrageenan-induced rat paw edema test and all of the compounds were found to be equipotent to Diclofenac sodium in the acetic acid induced writhing analgesic model. Out of six derivatives two derivatives found to produce no ulceration in stomach specimen of rats; nitric oxide seems to contribute to their excellent safety profile which supports several endogenous GIT defense mechanisms, including increase in mucus, bicarbonate secretions, increase in mucosal blood flow, and inhibition of the activation of pro-inflammatory cells by which NO-Indomethacin protects GI mucosa.

Keywords: Indomethacin, NO-donor, non-ulcerogenic, NSAIDs, 1-(2-(Benzoyl-Substituted-2-phenyl-1H-Indol-5-Carbony) Hydrazinyloxy) Vinyl Nitrate Derivatives, anti-inflammatory, analgesic, ulcerogenic properties, Diclofenac sodium, edema test, bicarbonate secretions, GIT defense mechanisms, pro-inflammatory cells, NO-Indomethacin, Non-steroidal anti-inflammatory drugs, cy-clooxygenase enzymes, Ibuprofen, Diclofenac, Naproxen, Aspirin, Glafenine, Floctafenine, prostaglandin biosynthesis, 5-Lipoxygenase, cyclooxy-genase-2, COX-2 inhibitors, nitric oxide, Rofecoxib, Nitro-aspirin, Nitro-naproxen, Nitro-Ketoprofen, Nitro-ibuprofen, furoxans, oximes, hydrazides, thionyl chloride, titrimetric assays, infrared spectrometer, Micro analytical Unit, National Center for Cell Science, Institutional Animal Ethical Committee, sodium carboxy methyl cellulose, plethysmometer, Dunnet's test, mucosal ulceration, Haema-toxylin and Eosin staining, Vasorelaxing Activity, di-methylsulfoxide, Griess reagent, carrageenan-induced rat paw edema method

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Article Details

VOLUME: 6
ISSUE: 4
Year: 2010
Page: [211 - 218]
Pages: 8
DOI: 10.2174/1573406411006040211
Price: $58

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