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

• Published in: Chinese chemical letters Vol. 21; no. 10; pp. 1149 - 1152
• Main Authors: Rajak, Harish, Behera, Chinmay K., Pawar, Rajesh S., Singour, Pradeep K., Kharya, Murli Dhar
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01-10-2010; SLT Institute of Pharmaceutical Sciences, Guru Ghasidas University Bilaspur-495 009, (C.G.), India%VNS Institute of Pharmacy Neelbud, Bhopal-462 044, (M.P.), India%Department of Pharmaceutical Sciences, Dr. H.S. Gour University, Sagar-470 003,(M.P.), India
• Subjects: 1,3,4-Thiadiazoles; Anticonvulsant activity; carba; Semicarbazones; 噻二唑; 抗惊厥活性; 抗癫痫; 构效关系; 结合位点; 缩氨脲; Anticonvulsant activity; 1,3,4-Thiadiazoles; Semicarbazones
• ISSN: 1001-8417; 1878-5964
• DOI: 10.1016/j.cclet.2010.04.012

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.