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
Letters in Drug Design & Discovery
Title: Synthesis and Anticonvulsant Activity of Some Cinnamylpiperazine Derivatives
Volume: 7 Issue: 9
Author(s): Chuan Hu, Zhi-Gang Sun, Cheng-Xi Wei and Zhe-Shan Quan
Affiliation:
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
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.
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Cite this article as:
Hu Chuan, Sun Zhi-Gang, Wei Cheng-Xi and Quan Zhe-Shan, Synthesis and Anticonvulsant Activity of Some Cinnamylpiperazine Derivatives, Letters in Drug Design & Discovery 2010; 7 (9) . https://dx.doi.org/10.2174/157018010792929595
DOI https://dx.doi.org/10.2174/157018010792929595 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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