Synthesis and Evaluation of In Vivo Anticonvulsant Activity of 2,5-Disubstituted-1,3,4-Oxadiazole Derivatives

被引:5
|
作者
Harish, Kikkeri P. [1 ]
Mohana, Kikkeri N. [1 ]
Mallesha, Lingappa [2 ]
Veeresh, B. [3 ]
Reddy, B. Madhava [3 ]
Kumar, Nagula Naresh [3 ]
机构
[1] Univ Mysore, Dept Studies Chem, Mysore 570006, Karnataka, India
[2] JSS Coll Arts Commerce & Sci, PG Dept Chem, Mysore 25, Karnataka, India
[3] G Pullareddy Coll Pharm, Dept Pharmacol & Toxicol, Hyderabad 28, Andhra Pradesh, India
关键词
Synthesis; 1,3,4-oxadiazole; Anticonvulsant activity; Neurotoxicity; Rotorod;
D O I
10.2174/15701808113109990020
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of new 2,5-disubstituted-1,3,4-oxadiazole derivatives 8(a-o) was synthesized by the reaction of 1-(5-phenyl-1,3,4-oxadiazol-2-yl)piperazine with various sulfonyl chlorides. The synthesized compounds were characterized by elemental analyses, H-1 NMR, C-13 NMR and mass spectral studies. The newly synthesized compounds were screened for their anticonvulsant activity against maximal electroshock (MES) seizure method and compared with the standard drug phenytoin. The neurotoxic effects were determined by rotorod test. Compounds 8d, 8e and 8f were found to be most potent of this series. The same compounds showed no neurotoxicity at the maximum dose administered (100 mg/kg). The efforts were also made to establish the structure activity relationships among synthesized compounds.
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页码:783 / 791
页数:9
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