Synthesis and biological evaluation of a new class of benzothiazines as neuroprotective agents

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• 作者：Alessandra Mancini^a ; Alessia Chelini^a ; Angela Di Capua^a ; ^b ; Loretta Castelli^c ; Simone Brogi^a ; Marco Paolino^a ; Germano Giuliani^a ; Andrea Cappelli^a ; Maria Frosini^d ; Lorenzo Ricci^d ; Erminia Leonelli^d ; Gianluca Giorgi^a ; Antonio Giordani^e ; Jacopo Magistretti^c ; Maurizio Anzini^a ; ^{maurizio.anzini@unisi.it}
• 关键词：Neuroprotective agents ; Neurodegenerative diseases ; Benzothiazine derivatives ; SH-SY5Y cells ; Neuronal voltage-dependent Na+ and Ca2+ currents
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：614-630
• 全文大小：2556 K
• 卷排序：126

文摘

Synthesis and biological evaluation of new benzothiazines as neuroprotective agents. Derivatives 5b-d can reduce glutamate and LDH release. 5b-d reduce glutamate- and 6-OHDA-induced cytotoxicity and limit ROS formation. 5c proved effective in inhibiting neuronal voltage-dependent Na+ and Ca2+-channels.