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Design, synthesis and biological evaluation of 4,5-dibromo-N-(thiazol-2-yl)-1H-pyrrole-2-carboxamide derivatives as novel DNA gyrase inhibitorsTomašič, Tihomir ...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.Source: Bioorganic & Medicinal Chemistry. - ISSN 0968-0896 (Vol. 25, iss. 1, 2017, str. 338-349)Type of material - article, component part ; adult, seriousPublish date - 2017Language - englishCOBISS.SI-ID - 4240753
Author
Tomašič, Tihomir |
Mirt, Matic |
Barančokova, Michaela |
Ilaš, Janez |
Zidar, Nace |
Tammela, Päivi |
Kikelj, Danijel
Topics
antibacterial |
DNA gyrase |
docking |
inhibitor |
thiazole
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Tomašič, Tihomir | 28334 |
Mirt, Matic | ![]() |
Barančokova, Michaela | 39784 |
Ilaš, Janez | 24400 |
Zidar, Nace | 28905 |
Tammela, Päivi | ![]() |
Kikelj, Danijel | 01463 |
Source: Personal bibliographies
and: SICRIS
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