Synthesis of Novel 1-benzhydryl-4-(3-(piperidin-4-yl)propyl) Piperidine Sulfonamides as Anticonvulsant Agents

被引：4
|
作者：
Vinaya, K. [1 ]
Veeresh, B. [2 ]
Kumar, C. S. Ananda [1 ]
Prasanna, D. S. [1 ]
Ranganatha, S. R. [1 ]
Prasad, S. B. Benaka [1 ]
Patil, B. M. [3 ]
Rangappa, K. S. [1 ]
机构：
[1] Univ Mysore, Dept Studies Chem, Mysore 570006, Karnataka, India
[2] KLESs Coll Pharm, Dept Pharmacol, Belgaum 590010, India
[3] KLESs Coll Pharm, Dept Pharmacol, Vijayanagar 580031, Hubli, India
来源：
LETTERS IN DRUG DESIGN & DISCOVERY | 2010年 / 7卷 / 02期
关键词：
Benzhydryl chloride; Sulfonyl chloride; Anticonvulsant; Convulsiometer; Epilepsy; DESIGN; ESTERS;
D O I：
10.2174/157018010790225868
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of novel 1-benzhydryl-4-(3-(piperidin-4-yl)propyl)piperidine sulphonamide derivatives 8(a-j) was synthesized in good yield and met the structural requirements essential for anticonvulsant properties. The structures of the synthesized compounds were confirmed on the basis of their spectral data and elemental analysis. All the compounds were evaluated for their possible anticonvulsant activity by Maximal Electroshock Seizure (MES) test and their neurotoxic effects were determined by rotorod test. Majority of the compounds were active in MES tests. Compounds 8f and 8g have shown a significant and protective effect on seizure, when compared with standard drug phenytoin. Compound 8f and 8g without a fluoro group showed anticonvulsant activity in MES test as compared with compound 8a and 8b with fluoro substituents. From this study, it is quite apparent that there are at least three parameters for the activity of anticonvulsant drugs, that is, a lipophilic domain, a distal hydrophobic center and two-electron donor (-C-N-) system.
引用
收藏
页码：109 / 115
页数：7
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