Discovery of Benzothiazole Scaffold-Based DNA Gyrase B Inhibitors

• Published in: Journal of medicinal chemistry Vol. 59; no. 19; pp. 8941 - 8954
• Main Authors: Gjorgjieva, Marina, Tomašič, Tihomir, Barančokova, Michaela, Katsamakas, Sotirios, Ilaš, Janez, Tammela, Päivi, Peterlin Mašič, Lucija, Kikelj, Danijel
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 13.10.2016; Amer Chemical Soc
• Subjects: Anti-Bacterial Agents - chemistry; Anti-Bacterial Agents - pharmacology; Benzothiazoles - chemistry; Benzothiazoles - pharmacology; Chemistry, Medicinal; Crystallography, X-Ray; DNA Gyrase - metabolism; DNA Topoisomerase IV - antagonists & inhibitors; DNA Topoisomerase IV - metabolism; Drug Design; Escherichia coli - drug effects; Escherichia coli - enzymology; Escherichia coli Infections - drug therapy; Escherichia coli Infections - microbiology; Humans; Life Sciences & Biomedicine; Models, Molecular; Pharmacology & Pharmacy; Science & Technology; Staphylococcal Infections - drug therapy; Staphylococcal Infections - microbiology; Staphylococcus aureus - drug effects; Staphylococcus aureus - enzymology; Structure-Activity Relationship; Topoisomerase II Inhibitors - chemistry; Topoisomerase II Inhibitors - pharmacology; DESIGN; POTENT; ATPASE INHIBITORS; CRYSTAL-STRUCTURE; ESCHERICHIA-COLI; QUINOLONES; CYCLOTHIALIDINES; TOPOISOMERASE-IV; N-PHENYL-4,5-DIBROMOPYRROLAMIDES; N-PHENYLINDOLAMIDES

Bacterial DNA gyrase and topoisomerase IV control the topological state of DNA during replication and are validated targets for antibacterial drug discovery. Starting from our recently reported 4,5,6,7-tetrahydro­benzo­[1,2-d]­thiazole-based DNA gyrase B inhibitors, we replaced their central core wi...