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Download filePractical Synthesis and Application of Halogen-Doped Pyrrole Building Blocks
journal contribution
posted on 2021-03-30, 17:33 authored 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 KikeljA 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.