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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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http://www.sciencedirect.com/science/article/pii/S0968089616310938
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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
UDC:
543:615.015.8
ISSN on article:
0968-0896
DOI:
10.1016/j.bmc.2016.10.038
COBISS.SI-ID:
4240753
Publication date in RUL:
09.03.2019
Views:
1840
Downloads:
1056
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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
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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