In:
Archiv der Pharmazie, Wiley, Vol. 350, No. 8 ( 2017-08)
Abstract:
The discovery and synthesis of new tyrosine‐based inhibitors of DNA gyrase B (GyrB), which target its ATPase subunit, is reported. Twenty‐four compounds were synthesized and evaluated for activity against DNA gyrase and DNA topoisomerase IV. The antibacterial properties of selected GyrB inhibitors were demonstrated by their activity against Staphylococcus aureus and Enterococcus faecalis in the low micromolar range. The most promising compounds, 8a and 13e , inhibited Escherichia coli and S. aureus GyrB with IC 50 values of 40 and 30 µM. The same compound also inhibited the growth of S. aureus and E. faecalis with minimal inhibitory concentrations (MIC 90 ) of 14 and 28 µg/mL, respectively.
Type of Medium:
Online Resource
ISSN:
0365-6233
,
1521-4184
DOI:
10.1002/ardp.201700087
Language:
English
Publisher:
Wiley
Publication Date:
2017
detail.hit.zdb_id:
1496815-0
detail.hit.zdb_id:
6381-2
SSG:
15,3
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