Novel derivatives of nitro-substituted salicylic acids: Synthesis, antimicrobial activity and cytotoxicity
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F71009396%3A_____%2F15%3AN0000007" target="_blank" >RIV/71009396:_____/15:N0000007 - isvavai.cz</a>
Alternative codes found
RIV/00216208:11160/15:10312619
Result on the web
<a href="https://www.sciencedirect.com/science/article/pii/S0968089615301085" target="_blank" >https://www.sciencedirect.com/science/article/pii/S0968089615301085</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.bmc.2015.10.029" target="_blank" >10.1016/j.bmc.2015.10.029</a>
Alternative languages
Result language
angličtina
Original language name
Novel derivatives of nitro-substituted salicylic acids: Synthesis, antimicrobial activity and cytotoxicity
Original language description
Inspired by the high antituberculous activity of novel nitro-substituted derivatives and based on promising predicted ADMET properties we have synthesized a series of 33 salicylanilides containing nitro-group in their salicylic part and evaluated them for their in vitro antimycobacterial, antimicrobial and antifungal activities. The presence of nitro-group in position 4 of the salicylic acid was found to be beneficial and the resulting molecules exhibited minimum inhibitory concentrations (MICs) ranging from 2 to 32 mu M against Mycobacterium tuberculosis. The best activity was found for 2-hydroxy-4-nitro-N-[4-(trifluoromethyl)phenyl] benzamide (MIC = 2 mu M). 4-Nitrosalicylanilides were also found to be active against all Staphylococcus species tested while for MRSA strain 2-hydroxy-4-nitro-N-[4-(trifluoromethyl)phenyl] benzamide's MIC was 0.98 mu M. None of the nitrosalicylanilides was active against Enterococcus sp. J 14365/08 and no considerable activity was found against Gram-negative bacteria or fungi. The hepatotoxicity of all nitrosalicylanilides was found to be in the range of their MICs for HepG2 cells. (C) 2015 Elsevier Ltd. All rights reserved.
Czech name
—
Czech description
—
Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
—
OECD FORD branch
30104 - Pharmacology and pharmacy
Result continuities
Project
—
Continuities
V - Vyzkumna aktivita podporovana z jinych verejnych zdroju
Others
Publication year
2015
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Bioorganic and Medicinal Chemistry
ISSN
0968-0896
e-ISSN
—
Volume of the periodical
23
Issue of the periodical within the volume
22
Country of publishing house
GB - UNITED KINGDOM
Number of pages
10
Pages from-to
7292-7301
UT code for WoS article
000364845500019
EID of the result in the Scopus database
2-s2.0-84946206735