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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 inhibitors
ID Tomašič, Tihomir (Author), ID Mirt, Matic (Author), ID Barančokova, Michaela (Author), ID Ilaš, Janez (Author), ID Zidar, Nace (Author), ID Tammela, Päivi (Author), ID Kikelj, Danijel (Author)

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Abstract
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.

Language:English
Keywords:antibacterial, DNA gyrase, docking, inhibitor, thiazole
Work type:Scientific work
Typology:1.01 - Original Scientific Article
Organization:FFA - Faculty of Pharmacy
Publication status:Published
Publication version:Author Accepted Manuscript
Year:2017
Number of pages:Str. 338-349
Numbering:Vol. 25, iss. 1
PID:20.500.12556/RUL-106639 This link opens in a new window
UDC:543:615.015.8
ISSN on article:0968-0896
DOI:10.1016/j.bmc.2016.10.038 This link opens in a new window
COBISS.SI-ID:4240753 This link opens in a new window
Publication date in RUL:09.03.2019
Views:1626
Downloads:1020
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Record is a part of a journal

Title:Bioorganic & medicinal chemistry
Shortened title:Bioorg. med. chem.
Publisher:Elsevier
ISSN:0968-0896
COBISS.SI-ID:756527 This link opens in a new window

Licences

License:CC BY-NC-ND 4.0, Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International
Link:http://creativecommons.org/licenses/by-nc-nd/4.0/
Description:The most restrictive Creative Commons license. This only allows people to download and share the work for no commercial gain and for no other purposes.
Licensing start date:09.03.2019

Projects

Funder:EC - European Commission
Funding programme:H2020
Project number:642620
Name:Interdisciplinary Training Network for Validation of Gram-Negative Antibacterial Targets
Acronym:INTEGRATE

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