Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Synthesis and Anticonvulsant Activity of Some Cinnamylpiperazine Derivatives

Author(s): Chuan Hu, Zhi-Gang Sun, Cheng-Xi Wei, Zhe-Shan Quan.

Abstract:

A series of cinnamylpiperazine derivatives was synthesized using different benzophenone as starting material. The structures of the compounds were proved by their IR, 1H-NMR spectroscopic data and mass spectra data. The anticonvulsant activities of these compounds were evaluated with maximal electroshock (MES) test and rotarod test with intraperitoneal injection on KunMing mice. Among all the flunarizine analogues, no one exhibited better anticonvulsant activity than flunarizine. Flunarizine (4i) exhibited anticonvulsant activity with ED50 of 38.1 mg/kg, TD50 of 164.3 mg/kg and PI of 4.3 through administration intraperitoneal, and with ED50 of 56.8 mg/kg, TD50 of 456.3 mg/kg and PI of 8.0 through oral administration.

Keywords: Anticonvulsant, MES, Calcium channel, Flunarizine, Cinnarizine, Cinnamyl piperazine, Anticonvulsant activity, Cinnamylpiperazine Derivatives, Refractory childhood epilepsy, Structure activity relationship, Program (ADD), Drug Development, Intrinsic burst firing, Excitotoxic, Apoptotic cell, Pharmacology, Tonic maximal extension, Rotarod Test, Cinnarizine-induced parkinsonism

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Article Details

VOLUME: 7
ISSUE: 9
Year: 2010
Page: [661 - 664]
Pages: 4
DOI: 10.2174/157018010792929595
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