20.500.12556/RUL-106642 Synthesis and evaluation of N-phenylpyrrolamides as DNA gyrase B inhibitors ATP-competitive inhibitors of DNA gyrase and topoisomerase IV are among the most interesting classes of antibacterial drugs that are unrepresented in the antibacterial pipeline. We developed 32 new N-phenylpyrrolamides and evaluated them against DNA gyrase and topoisomerase IV from E. coli and Staphylococcus aureus. Antibacterial activities were studied against Gram-positive and Gram-negative bacterial strains. The most potent compound displayed an IC50 of 47micro nm against E.coli DNA gyrase, and a minimum inhibitory concentration (MIC) of 12.5 microm against the Gram-positive Enterococcus faecalis. Some compounds displayed good antibacterial activities against an efflux-pump-deficient E. coli strain (MIC=6.25 microm) and against wild-type E. coli in the presence of efflux pump inhibitor PAbetaN (MIC=3.13 microm). Here we describe new findings regarding the structure-activity relationships of N-phenylpyrrolamide DNA gyrase B inhibitors and investigate the factors that are important for the antibacterial activity of this class of compounds. DNA gyrase GyrB antibacterials inhibitors pyrrolamides true false true Angleški jezik Slovenski jezik Članek v reviji 2019-03-09 19:46:20 2019-03-09 19:46:21 2022-10-12 12:54:11 0000-00-00 00:00:00 2018 0 0 Str. 186-198 iss. 2 Vol. 13 2018 0000-00-00 Zaloznikova Objavljeno NiDoloceno 0000-00-00 0000-00-00 0000-00-00 2019-01-22 543.2/.9.057 1860-7187 10.1002/cmdc.201700549 4461681 RAZ_Durcik_Martina_i2018.pdf RAZ_Durcik_Martina_i2018.pdf 1 EBBC6FC6AD0AD83A0AF84B22FB2ED78A 796ea02315fa4a7b91b8584cadbb3daf23bb532559645a8231edb0bc7a50ed77 5cfed933-a1b6-11eb-a523-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=117456 https://onlinelibrary.wiley.com/doi/10.1002/cmdc.201700549 1 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=117436 Fakulteta za farmacijo 0 0 0