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Št. zadetkov: 2
Discovery and Hit-to-Lead Optimization of Benzothiazole scaffold-based DNA gyrase inhibitors with potent activity against Acinetobacter baumannii and Pseudomonas aeruginosa
Andrej Emanuel Cotman, Martina Durcik, Davide Benedetto Tiz, Federica Fulgheri, Maša Sterle, Štefan Možina, Žiga Skok, Nace Zidar, Anamarija Zega, Janez Ilaš, Lucija Peterlin-Mašič, Tihomir Tomašić, Danijel Kikelj
Izvirni znanstveni članek
Oznake: antibacterial activity;bacteria;genetics;inhibitors;solubility;
We have developed compounds with a promising activity against Acinetobacter baumannii and Pseudomonas aeruginosa, which are both on the WHO priority list of antibiotic-resistant bacteria. Starting from DNA gyrase inhibitor 1, we identified compound 27, featuring a 10-fold improved aqueous solubility ...
Leto: 2023 Vir: Fakulteta za farmacijo (UL FFA)
New N-phenylpyrrolamide inhibitors of DNA gyrase with improved antibacterial activity
Andrej Emanuel Cotman, Federica Fulgheri, Martina Piga, Peter Peršolja, Davide Benedetto Tiz, Žiga Skok, Martina Durcik, Maša Sterle, Jaka Dernovšek, Anamarija Zega, Lucija Peterlin-Mašič, Janez Ilaš, Tihomir Tomašić, Danijel Kikelj, Nace Zidar
Izvirni znanstveni članek
Oznake: N-fenilpirolamidni inhibitorji;bakterijske DNA giraze;sinteza spojin;antibakterijsko delovanje;
This study presents the discovery of a new series of N-phenylpyrrolamide inhibitors of bacterial DNA gyrase with improved antibacterial activity. The most potent inhibitors had low nanomolar IC50 values against Escherichia coli DNA gyrase (IC50; 2–20 nM) and E. coli topoisomerase IV (22i, IC50 = 143 ...
Leto: 2024 Vir: Fakulteta za farmacijo (UL FFA)
Št. zadetkov: 2
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