Antibacterial Drug Leads: DNA and Enzyme Multitargeting
Wei Zhu
1
,
Yang Wang
1
,
Kai Li
1
,
Jian GAO
2
,
Chun-Hsiang Huang
2
,
Chun Chi Chen
2
,
Tzu‑Ping Ko
3
,
Yong Zhang
1
,
Rey-Ting Guo
2
,
Publication type: Journal Article
Publication date: 2015-01-22
scimago Q1
wos Q1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
25574764
Drug Discovery
Molecular Medicine
Abstract
We report the results of an investigation of the activity of a series of amidine and bisamidine compounds against Staphylococcus aureus and Escherichia coli. The most active compounds bound to an AT-rich DNA dodecamer (CGCGAATTCGCG)2 and using DSC were found to increase the melting transition by up to 24 °C. Several compounds also inhibited undecaprenyl diphosphate synthase (UPPS) with IC50 values of 100-500 nM, and we found good correlations (R(2) = 0.89, S. aureus; R(2) = 0.79, E. coli) between experimental and predicted cell growth inhibition by using DNA ΔTm and UPPS IC50 experimental results together with one computed descriptor. We also solved the structures of three bisamidines binding to DNA as well as three UPPS structures. Overall, the results are of general interest in the context of the development of resistance-resistant antibiotics that involve multitargeting.
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52
Total citations:
52
Citations from 2025:
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(3.85%)
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GOST
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Zhu W. et al. Antibacterial Drug Leads: DNA and Enzyme Multitargeting // Journal of Medicinal Chemistry. 2015. Vol. 58. No. 3. pp. 1215-1227.
GOST all authors (up to 50)
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Zhu W., Wang Y., Li K., GAO J., Huang C., Chen C. C., Ko T., Zhang Y., Guo R., OLDFIELD E. Antibacterial Drug Leads: DNA and Enzyme Multitargeting // Journal of Medicinal Chemistry. 2015. Vol. 58. No. 3. pp. 1215-1227.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1021/jm501449u
UR - https://doi.org/10.1021/jm501449u
TI - Antibacterial Drug Leads: DNA and Enzyme Multitargeting
T2 - Journal of Medicinal Chemistry
AU - Zhu, Wei
AU - Wang, Yang
AU - Li, Kai
AU - GAO, Jian
AU - Huang, Chun-Hsiang
AU - Chen, Chun Chi
AU - Ko, Tzu‑Ping
AU - Zhang, Yong
AU - Guo, Rey-Ting
AU - OLDFIELD, ERIC
PY - 2015
DA - 2015/01/22
PB - American Chemical Society (ACS)
SP - 1215-1227
IS - 3
VL - 58
PMID - 25574764
SN - 0022-2623
SN - 1520-4804
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2015_Zhu,
author = {Wei Zhu and Yang Wang and Kai Li and Jian GAO and Chun-Hsiang Huang and Chun Chi Chen and Tzu‑Ping Ko and Yong Zhang and Rey-Ting Guo and ERIC OLDFIELD},
title = {Antibacterial Drug Leads: DNA and Enzyme Multitargeting},
journal = {Journal of Medicinal Chemistry},
year = {2015},
volume = {58},
publisher = {American Chemical Society (ACS)},
month = {jan},
url = {https://doi.org/10.1021/jm501449u},
number = {3},
pages = {1215--1227},
doi = {10.1021/jm501449u}
}
Cite this
MLA
Copy
Zhu, Wei, et al. “Antibacterial Drug Leads: DNA and Enzyme Multitargeting.” Journal of Medicinal Chemistry, vol. 58, no. 3, Jan. 2015, pp. 1215-1227. https://doi.org/10.1021/jm501449u.