Ontology highlight
ABSTRACT:
SUBMITTER: Durcik M
PROVIDER: S-EPMC7822030 | biostudies-literature | 2020 Dec
REPOSITORIES: biostudies-literature
Durcik Martina M Skok Žiga Ž Ilaš Janez J Zidar Nace N Zega Anamarija A Szili Petra Éva PÉ Draskovits Gábor G Révész Tamás T Kikelj Danijel D Nyerges Akos A Pál Csaba C Mašič Lucija Peterlin LP Tomašič Tihomir T
Pharmaceutics 20201222 1
The discovery of multi-targeting ligands of bacterial enzymes is an important strategy to combat rapidly spreading antimicrobial resistance. Bacterial DNA gyrase and topoisomerase IV are validated targets for the development of antibiotics. They can be inhibited at their catalytic sites or at their ATP binding sites. Here we present the design of new hybrids between the catalytic inhibitor ciprofloxacin and ATP-competitive inhibitors that show low nanomolar inhibition of DNA gyrase and antibacte ...[more]