Synthesis and evaluation of anti-inflammatory, analgesic, ulcerogenicity and nitric oxide-releasing studies of novel ibuprofen analogs as nonulcerogenic derivatives

Abstract

Since the last 41 years, Ibuprofen has been one of the most widely used Non-Steroidal Anti-Inflammatory Drug (NSAID) due to its anti-inflammatory actions. As all the NSAIDs are suffering from the deadlier GI toxicities, Ibuprofen also is no exception to these toxicities. The free -COOH group is thought to be responsible for the Gastrointestinal (GI) tract toxicity associated with all the traditional NSAIDs. Therefore, the main aim of this study was to develop new chemical entities as potential anti-inflammatory agents with less GI toxicities. In this article, synthesis of a series of Hybrid molecules containing important pharmacophore of Ibuprofen and substituted diaryl rings on 5-membered heterocycle similar to coxibs and Nitric oxidereleasing moiety are described. All the synthesized compounds were tested in vivo for their anti-inflammatory, analgesic, ulcerogenic properties, and histopathological studies and in vitro for their nitric oxide-releasing properties. Out of the six synthesized compounds, four compounds showed significant anti-inflammatory and analgesic activity which was compared with standard. All the synthesized compounds exhibited significant nitric oxide-releasing and reduced GI ulcerogenic activity.

PEG Mediated Synthesis and Biological Evaluation of Asymmetrical Pyrazole Curcumin Analogues as Potential Analgesic, Anti‐Inflammatory and Antioxidant Agents

“…The analgesic activity was evaluated using the acetic acid induced writhing method using groups of six animals each. A solution of acetic acid (1% v/v) in distilled water was prepared and injected intraperitoneally in a volume of 0.1 mL.…”

Peel Extract Associated Oxidative Green Dakin Synthesis of Some Phenols Using Aqueous Banana Extract Catalyst

“…In the continuation of our previous work [11][12][13][14][15][16][17][18][19][20][21][22][23] , it was confirmed that until now none of the methods had used such a mild and green catalyst and solvents for Dakin oxidation. The designed method is suitable for the conversion of substituted benzaldehydes to its consequent substituted phenols.…”

Synthesis and Pharmacological Evaluation of New Chemical Entities from Ibuprofen as Novel Analgesic Candidates

“…2. Ethyl-2-(alkylsulphonyloxy) alkanoates (6)(7)(8)(9)(10) were prepared according to the published method [24] using ethyl 2-hydroxyalkanoates and mesyl chloride (MsCl) in dry dichloromethane. Reaction of these intermediates with a mixture of various alkylbenzenes and AlCl 3 yielded ethyl 2-(4-alkylphenyl)-2-alkylalkanoates (14-20) was examined.…”