20.500.12556/RUL-106639 Design, synthesis and biological evaluation of 4,5-dibromo-N-(thiazol-2-yl)-1H-pyrrole-2-carboxamide derivatives as novel DNA gyrase inhibitors Development of novel DNA gyrase B inhibitors is an important field of antibacterial drug discovery whose aim is to introduce a more effective representative of this mechanistic class into the clinic. In the present study, two new series of Escherichia coli DNA gyrase inhibitors bearing the 4,5-dibromopyrrolamide moiety have been designed and synthesized. 4,5,6,7-Tetrahydrobenzo[1,2-d]thiazole-2,6-diamine derivatives inhibited E. coli DNA gyrase in the submicromolar to low micromolar range (IC50 values between 0.891 and 10.4 microM). Their ''ring-opened'' analogues, based on the 2-(2-aminothiazol-4-yl)acetic acid scaffold, displayed weaker DNA gyrase inhibition with IC50 values between 15.9 and 169 microM. Molecular docking experiments were conducted to study the binding modes of inhibitors. antibacterial DNA gyrase docking inhibitor thiazole true false true Angleški jezik Slovenski jezik Znanstveno delo 2019-03-09 19:16:43 2019-03-09 19:16:46 2022-08-19 03:46:36 0000-00-00 00:00:00 2017 0 0 Str. 338-349 iss. 1 Vol. 25 2017 0000-00-00 PostprintKoncna Objavljeno NiDoloceno 0000-00-00 0000-00-00 0000-00-00 2019-01-01 543:615.015.8 0968-0896 10.1016/j.bmc.2016.10.038 4240753 756527 RAZ_Tomasic_Tihomir_i2017.pdf RAZ_Tomasic_Tihomir_i2017.pdf 1 E03DD84A1FFD1F9D6F55E9128E923C5E 56829db1af9559ea0f0f54631071363e20b10e02844ed3c047671b49805d1317 5ccf3dde-a1b6-11eb-a523-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=117453 http://www.sciencedirect.com/science/article/pii/S0968089616310938 1 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=117433 Fakulteta za farmacijo 0 0 0