Lipophosphonoxins II: Design, Synthesis, and Properties of Novel Broad Spectrum Antibacterial Agents
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68378050%3A_____%2F17%3A00477671" target="_blank" >RIV/68378050:_____/17:00477671 - isvavai.cz</a>
Alternative codes found
RIV/61388971:_____/17:00477671 RIV/61388963:_____/17:00477671 RIV/00216208:11310/17:10367905 RIV/61989592:15110/17:73585895
Result on the web
<a href="http://dx.doi.org/10.1021/acs.jmedchem.7b00355" target="_blank" >http://dx.doi.org/10.1021/acs.jmedchem.7b00355</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1021/acs.jmedchem.7b00355" target="_blank" >10.1021/acs.jmedchem.7b00355</a>
Alternative languages
Result language
angličtina
Original language name
Lipophosphonoxins II: Design, Synthesis, and Properties of Novel Broad Spectrum Antibacterial Agents
Original language description
The increase in the number of bacterial strains resistant to known antibiotics is alarming. In this study we report the synthesis of novel compounds termed Lipophosphonoxins II (LPPO II). We show that LPPO II display excellent activities against Gram-positive and-negative bacteria, including pathogens and multiresistant strains. We describe their mechanism of action plasmatic membrane pore-forming activity selective for bacteria. Importantly, LPPO II neither damage nor cross the eukaryotic plasmatic membrane at their bactericidal concentrations. Further, we LPPO II have low propensity for resistance development, likely due to their rapid membrane-targeting mode of action. Finally, we reveal that LPPO II are not toxic to either eukaryotic cells or model animals when administered orally or topically. Collectively, these results suggest that LPPO II are highly promising compounds for development into pharmaceuticals.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10606 - Microbiology
Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2017
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Journal of Medicinal Chemistry
ISSN
0022-2623
e-ISSN
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Volume of the periodical
60
Issue of the periodical within the volume
14
Country of publishing house
US - UNITED STATES
Number of pages
21
Pages from-to
6098-6118
UT code for WoS article
000406727700011
EID of the result in the Scopus database
2-s2.0-85026387650