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Practical Synthesis and Application of Halogen-Doped Pyrrole Building Blocks

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journal contribution
posted on 30.03.2021, 17:33 by Andrej Emanuel Cotman, Thomas Guérin, Ivana Kovačević, Davide Benedetto Tiz, Martina Durcik, Federica Fulgheri, Štefan Možina, Daniela Secci, Maša Sterle, Janez Ilaš, Anamarija Zega, Nace Zidar, Lucija Peterlin Mašič, Tihomir Tomašič, Frédéric R. Leroux, Gilles Hanquet, Danijel Kikelj
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.

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