Tanaya Jati Dharma Dewi and Siswandono Siswodihardjo and Juni Ekowati (2017) Design, Synthesis and Analgesic Activity of 3-Chlorobenzoyl-N-(2-amino-4-chlorophenyl)anthranilic acid. International Journal of Pharmaceutical Chemistry, 7 (12). pp. 162-166. ISSN 2249-734X

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Abstract

Anthranilic acid derivatives such as a mefenamicacid arewell known as an analgesicdrug. Modification of anthranilic acid derivate was designed to get better analgesic activity. Docking studies were performed usingMolegro Virtual Docker 5.0 software with the proteintarget cyclooxygenase-2 receptor (PDB ID: 5IKR). The synthesiswas carried out by modification ScottenBaumannreaction via nucleophilic reaction of N-(2-amino-4-chlorophenyl)anthranilic acid and 3-chlorobenzoylchloride. Synthesized compound was characterizedby IR, 1H-NMR, 13C-NMR, Mass spectrometry. Biological activity for analgesicof the proposedcompoundby writhingtest methodon mice (Musmusculus). The resultfrom docking studies revealed that rerank score of 3-chlorobenzoyl-N-(2-amino-4-chlorophenyl) anthranilic acid get lower than mefenamic acid which related its higher analgesic activity. 3-Chlorobenzoyl-N-(2-amino-4-chlorophenyl)anthranilic acid showed better pain inhibition activity compare mefenamic acid with ED50= 30.443 mg/kgBW.This result gave a development of anthranilic acid derivate to be potential analgesic drug candidate.

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