Simple N,N-dimethyl phenylsulfonamides show potent anticonvulsant effect in two standard epilepsy models

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• 作者：Tomoyuki Tanaka ; ^{tomoyuki-1-tanaka@ds-pharma.co.jp} ; Nana Yajima ; Tomoko Kiyoshi ; Yoshiki Miura ; Seiji Iwama
• 关键词：Phenylsulfoneamide ; Epilepsy ; In vivo screening ; MES ; PTZ
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：1 January 2017
• 年：2017
• 卷：27
• 期：1
• 页码：94-97
• 全文大小：2104 K
• 卷排序：27

文摘

Optimization of the previously reported benzothiazine analogue A led to the identification of compound 1, which showed anti-convulsant activity in two golden standard animal models of seizure, the MES and scPTZ models. Structure-activity relationship investigation of compound 1 revealed compounds 2, 6 and 19 as attractive anti-epileptic drug (AED) candidates with potent anticonvulsant effect in both the MES and scPTZ models. As these compounds are structurally different from existing AEDs, determination of their mechanism of actions could provide clues to understanding current therapy-resistant seizures. Moreover, these simple phenylsulfoneamide compounds could be good starting points for searching broad spectrum AEDs by such in vivo screening.