A novel series of 2,5-disubstituted 1,3,4-thiadiazoles as potential anticonvulsant agent  

作　　者：Harish Rajak Chinmay K.Behera Raiesh S.Pawar Pradeep K.Singour Murli Dhar Kharya 

机构地区：[1]SLT Institute of Pharmaceutical Sciences,Guru Ghasidas University [2]VNS Institute of Pharmacy [3]Department of Pharmaceutical Sciences,Dr.H.S.Gour University

出　　处：《Chinese Chemical Letters》2010年第10期1149-1152,共4页中国化学快报（英文版）

摘　　要：In pursuit for better antiepileptic drug and the importance of semicarbazones and 2,5-disubstituted 1,3,4-thiadiazoles as anticonvulsant pharmacophore, a series of novel N-（{5-[（6-methyl-l-benzofuran-3-yl）methyl]-l,3,4-thiadiazol-2-yl}carba- mothioyl）-2/3/4-substitutedbenzamide were designed, synthesized and evaluated for their anticonvulsant activity. The findings of the present studies confirmed that the pharmacophore model with four binding sites is crucial for anticonvulsant activity. Structure-activity relationships among synthesized compounds were also established.In pursuit for better antiepileptic drug and the importance of semicarbazones and 2,5-disubstituted 1,3,4-thiadiazoles as anticonvulsant pharmacophore, a series of novel N-（{5-[（6-methyl-l-benzofuran-3-yl）methyl]-l,3,4-thiadiazol-2-yl}carba- mothioyl）-2/3/4-substitutedbenzamide were designed, synthesized and evaluated for their anticonvulsant activity. The findings of the present studies confirmed that the pharmacophore model with four binding sites is crucial for anticonvulsant activity. Structure-activity relationships among synthesized compounds were also established.

关 键 词：1 3 4-Thiadiazoles SEMICARBAZONES Anticonvulsant activity 

分 类 号：O626[理学—有机化学]