卤素掺杂吡咯结构单元的实际合成与应用
Practical Synthesis and Application of Halogen-Doped Pyrrole Building Blocks.
作者信息
Cotman Andrej Emanuel, Guérin Thomas, Kovačević Ivana, Benedetto Tiz Davide, Durcik Martina, Fulgheri Federica, Možina Štefan, Secci Daniela, Sterle Maša, Ilaš Janez, Zega Anamarija, Zidar Nace, Mašič Lucija Peterlin, Tomašič Tihomir, Leroux Frédéric R, Hanquet Gilles, Kikelj Danijel
机构信息
Faculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.
Université de Strasbourg, CNRS, UMR 7042-LIMA, ECPM, 25 Rue Becquerel, Strasbourg 67087, France.
出版信息
ACS Omega. 2021 Mar 30;6(14):9723-9730. doi: 10.1021/acsomega.1c00331. eCollection 2021 Apr 13.
A practical access to four new halogen-substituted pyrrole building blocks was realized in two to five synthetic steps from commercially available starting materials. The target compounds were prepared on a 50 mg to 1 g scale, and their conversion to nanomolar inhibitors of bacterial DNA gyrase B was demonstrated for three of the prepared building blocks to showcase the usefulness of such chemical motifs in medicinal chemistry.
从市售起始原料出发，通过两到五步合成步骤，实现了四种新型卤素取代吡咯结构单元的实用合成方法。目标化合物的制备规模为50毫克至1克，并且对于所制备的三种结构单元，证明了它们可转化为细菌DNA促旋酶B的纳摩尔级抑制剂，以展示此类化学基序在药物化学中的实用性。
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