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Practical Synthesis and Application of Halogen-Doped Pyrrole Building Blocks.

ABSTRACT: 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.

SUBMITTER: Cotman AE

PROVIDER: S-EPMC8047689 | biostudies-literature | 2021 Apr

REPOSITORIES: biostudies-literature

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Practical Synthesis and Application of Halogen-Doped Pyrrole Building Blocks.

Cotman Andrej Emanuel AE Guérin Thomas T Kovačević Ivana I Benedetto Tiz Davide D Durcik Martina M Fulgheri Federica F Možina Štefan Š Secci Daniela D Sterle Maša M Ilaš Janez J Zega Anamarija A Zidar Nace N Mašič Lucija Peterlin LP Tomašič Tihomir T Leroux Frédéric R FR Hanquet Gilles G Kikelj Danijel D

ACS omega 20210330 14

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. ...[more]

PMID: 33869952

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