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 Evaluation of 6-phenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines

Author(s): Ming-Xia Song, Chun-Bo Zhang, Xian-Qing Deng, Zhi-Gang Sun, Zhe-Shan Quan.

Abstract:

Various 6-phenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine derivatives (3a-3n) were designed keeping in view the wide bioactivities of 1,2,4-triazoles and their fused heterocyclic derivatives. All target compounds 3a-3n, characterized by IR, 1H-NMR and MS, have been evaluated for their anticonvulsant activity against MES-induced seizures. The pharmacological results showed that most of the compounds displayed some degree of anticonvulsant activity. Among them, 6-(4-chlorophenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine (3h) was the most promising compound with an ED50 value of 40.9 mg/kg and a PI value of 6.5.

Keywords: Anticonvulsant, 1,2,4-Triazole, [1,3,4]Thiadiazine, Maximal electroshock test, Neurotoxicity, triazoles, epilepsy, antimicrobial, anticancer, nucleophilic centers, N-bridged heterocycles, phenacyl bromides, H-NMR, pharmacological testing, Elemental analyses

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Article Details

VOLUME: 8
ISSUE: 8
Year: 2011
Page: [769 - 773]
Pages: 5
DOI: 10.2174/157018011796575962
Price: $58