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Letters in Drug Design & Discovery

Author(s): Chuan-Feng Liu, Hong-Jian Zhang and Zhe-Shan Quan

DOI: 10.2174/1570180813666160324173717

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Synthesis and Anticonvulsant Activity of Novel 3-(2-(4H-1,2,4-triazol-4- yl)ethyl)-1-alkyl-1H-indole Derivatives

Page: [833 - 839] Pages: 7

  • * (Excluding Mailing and Handling)

Abstract

A series of novel 3-[2-(4H-1,2,4-triazol-4-yl)ethyl]-1-alkyl-1H-indole derivatives (4a-s) were synthesized and evaluated for their anticonvulsant activity and neurotoxicity by using maximal electroshock (MES) and rotarod neurotoxicity (TOX) tests. Among the compounds studied, compound 3-[2-(4H-1,2,4-triazol-4-yl)ethyl]-1-nonyl-1H-indole (4p) was found by intraperitoneal (i.p.) administration in mice to be the most potent compound with a median effective dose (ED50) value of 10.2 mg/kg, possessed better anticonvulsant activity and higher safety than carbamazepine.

Keywords: Synthesis, anticonvulsant, triazole, indole, maximal electroshock.

Graphical Abstract