Discovery and Hit-to-Lead Optimization of Benzothiazole Scaffold-Based DNA Gyrase Inhibitors with Potent Activity against Acinetobacter baumannii and Pseudomonas aeruginosa

[Image: see text] 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...

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Detalles Bibliográficos
Autores principales: Cotman, Andrej Emanuel, Durcik, Martina, Benedetto Tiz, Davide, Fulgheri, Federica, Secci, Daniela, Sterle, Maša, Možina, Štefan, Skok, Žiga, Zidar, Nace, Zega, Anamarija, Ilaš, Janez, Peterlin Mašič, Lucija, Tomašič, Tihomir, Hughes, Diarmaid, Huseby, Douglas L., Cao, Sha, Garoff, Linnéa, Berruga Fernández, Talía, Giachou, Paraskevi, Crone, Lisa, Simoff, Ivailo, Svensson, Richard, Birnir, Bryndis, Korol, Sergiy V., Jin, Zhe, Vicente, Francisca, Ramos, Maria C., de la Cruz, Mercedes, Glinghammar, Björn, Lenhammar, Lena, Henderson, Sara R., Mundy, Julia E. A., Maxwell, Anthony, Stevenson, Clare E. M., Lawson, David M., Janssen, Guido V., Sterk, Geert Jan, Kikelj, Danijel
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2023
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9884090/
https://www.ncbi.nlm.nih.gov/pubmed/36634346
http://dx.doi.org/10.1021/acs.jmedchem.2c01597

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