Design, synthesis and biological evaluation of 4,5-dibromo-N-(thiazol-2-yl)-1H-pyrrole-2-carboxamide derivatives as novel DNA gyrase inhibitors

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• 作者：Tihomir Toma&scaron ; ič^a ; ^{tihomir.tomasic@ffa.uni-lj.si} ; Matic Mirt^a ; Michaela Barančoková ; ^a ; Janez Ila&scaron ; ^a ; Nace Zidar^a ; Pä ; ivi Tammela^b ; Danijel Kikelj^a
• 关键词：Antibacterial ; DNA gyrase ; Docking ; Inhibitor ; Thiazole
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：1 January 2017
• 年：2017
• 卷：25
• 期：1
• 页码：338-349
• 全文大小：1248 K
• 卷排序：25

文摘

New 4,5-dibromopyrrolamides were prepared as ATPase inhibitors of DNA gyrase. Compounds were evaluated against Escherichia coli DNA gyrase in supercoiling assay. The most potent compound had an IC50 of 891 nM against E. coli DNA gyrase. Binding modes of inhibitors were studied by molecular docking.