Arzneimittelforschung 2012; 62(08): 372-377
DOI: 10.1055/s-0032-1314821
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Synthesis and Studies on the Anticonvulsant Activity of 5-alkoxy-[1,2,4]triazolo[4,3-a]pyridine Derivatives

L.-P. Guan
1   School of Food, Drug & Medicine Zhejiang Ocean University, Zhejiang, Zhoushan, China
,
R.-P. Zhang
2   College of Pharmacy, Yanbian University, Yanji, Jili, China
,
Y. Sun
1   School of Food, Drug & Medicine Zhejiang Ocean University, Zhejiang, Zhoushan, China
,
Y. Chang
2   College of Pharmacy, Yanbian University, Yanji, Jili, China
,
X. Sui
3   Qilu Pharmaceutical L CO.,LTD. Jinan City, China
› Author Affiliations
Further Information

Publication History

received 31 December 2011

accepted 02 May 2012

Publication Date:
10 July 2012 (online)

Abstract

In this study, a series of new 5-alkoxy-[1,2,4]triazolo[4,3-a]pyridine derivatives was synthesized and their anticonvulsant activity and neurotoxicity was evaluated with the maximal electroshock and rotarod tests, respectively. The most promising compounds, 3p (5-(4-chlorophenoxy)-[1,2,4]triazolo[4,3-a]pyridine) and 3r (5-(4-bromophenoxy)-[1,2,4]triazolo[4,3-a]pyridine), showed a median effective dose of 13.2 and 15.8 mg/kg and had a protective index value of 4.8 and 6.9, respectively. For exploring the putative mechanism of action, compounds 3n, 3p and 3r were tested in chemically induced models.