原创力文档discovery of substituted oxadiazoles as a novel scaffold for dna gyrase inhibitors：（发现取代恶二唑作为一种新型脚手架dna促旋酶抑制剂）.pdfVIP
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discovery of substituted oxadiazoles as a novel scaffold for dna gyrase inhibitors：（发现取代恶二唑作为一种新型脚手架dna促旋酶抑制剂）
European Journal of Medicinal Chemistry 130 (2017) 171e184
Contents lists available at ScienceDirect
European Journal of Medicinal Chemistry
journal homepage: /locate/ejmech
Research paper
Discovery of substituted oxadiazoles as a novel scaffold for DNA gyrase
inhibitors
a, * a a b € c
Ziga Jakopin , Janez Ilas , Michaela Barancokova , Matjaz Brvar , Paivi Tammela ,
a a a
Marija Sollner Dolenc , Tihomir Tomasic , Danijel Kikelj
a
University of Ljubljana, Faculty of Pharmacy, Askerceva 7, 1000 Ljubljana, Slovenia
b National Institute of Chemistry, Laboratory for Molecular Modeling, Hajdrihova ulica 19, 1001 Ljubljana, Slovenia
c University of Helsinki, Faculty of Pharmacy, Division of Pharmaceutical Biosciences, P.O. Box 56, FI-00014 Helsinki, Finland
a r t i c l e i n f o a b s t r a c t
Article history: DNA gyrase and topoisomerase IV are type IIa topoisomerases that are essential bacterial enzymes
Received 2 February 2017 required to oversee the topological state of DNA during transcription and replication processes. Their
Received in revised form ATPase domains, GyrB and ParE, respectively, are recognized as viable targets for small molecule in-
13 February 2017
hibitors, however, no synthetic or natural product GyrB/ParE inh
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