Preparation and In Vivo Antinociceptive Behavior of Four New 2‐Amino‐6‐trifuromethoxybenzothiazole Carboxylic Acid Derivatives. Issue 34 (9th September 2019)

• Record Type: Journal Article
• Authors: Wu, Xianglong; Wang, Qingchuan; Zhang, Fei; Liu, Hao; Lu, Tingli; Zhang, Qichun
• Is Part Of: ChemistrySelect. Volume 4:Issue 34(2019)
• Page Start: 9993
• Page End: 9998
• Publication Date: 2019-09-09
• Subjects: Antinociceptive -- Benzothiazole derivatives -- Carboxylic acids -- Heterocycles -- Riluzole; Chemistry -- Periodicals; 540.5
• DOI: 10.1002/slct.201902921
• Languages: English
• ISSNs: 2365-6549

Abstract

Abstract: Four novel N ‐substituted riluzole derivatives (4 a ‐4 d ) have been prepared and characterized. Their antinociceptive activities have been carefully investigated by hot‐plate test and writhing test. Our results indicated that at dose of 18 mg kg −1, 2‐( N ‐propionic acid)‐6‐trifluoromethoxy‐benzothiazole (4 a ), 2‐( N ‐butanoic acid)‐6‐trifluoromethoxy‐benzothiazole (4 b ) and 2‐( N ‐n‐caproic acid)‐6‐trifluoromethoxy‐benzothiazole (4 c ) significantly increased the nociceptive response latency under hot plate test while chemical nociception induced by intraperitoneal acetic acid was significantly inhibited by4 a and 2‐( N ‐proline)‐6‐trifluoromethoxy‐benzothiazole (4 d ) at same dosage. Our research clearly indicates that N ‐substituted Riluzole derivatives could be new alternative candidates as potential antinociceptive medicines. Abstract : Four new N ‐substituted carboxylic acid derivatives of Riluzole had been synthesized. The ultraviolet spectral properties, solubility test and Log P were studied. Antinociceptive activities were evaluated on the thermal nociception and on the chemical nociception. They have potential application in developing new drug candidates with antinociceptive activity.