TY - T1 - Exploring the Chemical Space of Benzothiazole-Based DNA Gyrase B Inhibitors SN - / UR - http://hdl.handle.net/10138/335330 T3 - A1 - Skok, Žiga; Barančoková, Michaela; Benek, Ondřej; Cruz, Cristina Durante; Tammela, Päivi; Tomašič, Tihomir; Zidar, Nace; Mašič, Lucija Peterlin; Zega, Anamarija; Stevenson, Clare E. M.; Mundy, Julia E. A.; Lawson, David M.; Maxwell, Anthony; Kikelj, Danijel; Ilaš, Janez A2 - PB - Y1 - 2020 LA - eng AB - We designed and synthesized a series of inhibitors of the bacterial enzymes DNA gyrase and DNA topoisomerase IV, based on our recently published benzothiazole-based inhibitor bearing an oxalyl moiety. To improve the antibacterial activity and retain potent enzymatic activity, we systematically explored the chemical space. Several strategies of modification were followed: varying substituents on the pyrrole carboxamide moiety, alteration of the central scaffold, including variation of substitutio... VO - IS - SP - OP - KW - 317 Pharmacy; DNA gyrase; topoisomerase IV; GyrB; ParE; antibacterial; benzothiazole; ANTIBACTERIAL ACTIVITY; N-PHENYLINDOLAMIDES; ATPASE INHIBITORS; DRUG DISCOVERY; KIBDELOMYCIN; N-PHENYL-4,5-DIBROMOPYRROLAMIDES; TRANSLOCATION; AMYCOLAMICIN; CHALLENGES; RESISTANCE; DNA gyrase; topoisomerase IV; GyrB; ParE; antibacterial; benzothiazole; ANTIBACTERIAL ACTIVITY; N-PHENYLINDOLAMIDES; ATPASE INHIBITORS; DRUG DISCOVERY; KIBDELOMYCIN; N-PHENYL-4,5-DIBROMOPYRROLAMIDES; TRANSLOCATION; AMYCOLAMICIN; CHALLENGES; RESISTANCE N1 - PP - ER -