TY  -  
T1  - Exploring the Chemical Space of Benzothiazole-Based DNA Gyrase B Inhibitors 
SN  -  /  
UR  - http://hdl.handle.net/10138/335330 
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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... 
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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 
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