Evaluation of Analgesic and Antiplatelet Activity of 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid

Publication date: Available online 26 July 2019Source: Prostaglandins & Other Lipid MediatorsAuthor(s): Caroline, Kuncoro Foe, Senny Yesery Esar, Ami Soewandi, Hevi Wihadmadyatami, Ratna Megawati Widharna, Wahyu Dewi Tamayanti, Elisabeth Kasih, Yudy TjahjonoAbstractsAcetylsalicylic acid is used as a non-steroidal anti-inflammatory drugs (NSAID) and antiplatelet agents by inhibiting cyclooxygenases. However, therapy using acetylsalicylic acid could induce gastric bleeding and cause other gastrointestinal toxicity. The aim of this study was to demonstrate the synthesis of a new compound bearing salicylic acid residue namely 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid, to analyze its potential as a ligand for human cyclooxygenase-2 (COX-2) receptor, to evaluate its toxicity level and its effectiveness for analgesic and antiplatelet agent compared with acetylsalicylic acid.Synthesis of 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid was conducted by microwave irradiation. The purity of this compound was evaluated with TLC, IR, NMR, and EDS spectroscopy. The chemical characterization and docking studies against human COX-2 (PDB:5F1A) was performed in-silico. The acute oral toxicity assay was performed under OECD guidelines. The analgesic activity study was performed by plantar and writhing test on animal model. For anti-platelet activity study, we performed tail-bleeding assay and flow cytometry based platelet aggregation assay. We could successfully synthesize a pure white crystall...
Source: Prostaglandins and Other Lipid Mediators - Category: Lipidology Source Type: research