Practical Synthesis and Application of Halogen-Doped
Pyrrole Building Blocks

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

doi:10.1021/acsomega.1c00331.s001

ao1c00331_si_001.pdf (2.93 MB)

Practical 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 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.