Design, synthesis and antimicrobial activities of thiouracil derivatives containing triazolo-thiadiazole as SecA inhibitors

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• 作者：Penglei Cui^a ; ^b ; Xiaoliu Li^a ; ^lixl@hbu.cn ; Mengyuan Zhu^c ; Binghe Wang^c ; Jing Liu^d ; Hua Chen^a ; ^{hua-todd@163.com}
• 关键词：Antibacterial activity ; SecA inhibitors ; Thiouracil ; Triazolo-thiadiazole ; Molecular simulation
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：159-165
• 全文大小：731 K
• 卷排序：127

文摘

Novel thiouracil derivatives containing a triazolo-thiadiazole moiety were synthesized. Most of the compounds showed strong antibacterial activities. Compound 7d significantly inhibited SecA ATPase activity. Compound 7d binds at a pocket close to the ATP-binding domain. The triazole-thiadiazole moiety was of benefit to their SecA inhibitory activity.