Practical Synthesis and Application of Halogen-Doped Pyrrole Building Blocks

Andrej Emanuel Cotman , Thomas Guérin (1) , 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 (1) , Gilles Hanquet (1) , Danijel Kikelj

1 LIMA - Laboratoire d'innovation moléculaire et applications

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.

Domaines: Chimie

Andrej Emanuel Cotman, Thomas Guérin, Ivana Kovačević, Davide Benedetto Tiz, Martina Durcik, et al.. Practical Synthesis and Application of Halogen-Doped Pyrrole Building Blocks. ACS Omega, 2021, 6 (14), pp.9723-9730. ⟨10.1021/acsomega.1c00331⟩. ⟨hal-03228819⟩