Synthesis and antimicrobial activity of sulphamethoxazole-based ureas and imidazolidine-2,4,5-triones

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11150%2F15%3A10312631" target="_blank" >RIV/00216208:11150/15:10312631 - isvavai.cz</a>
Alternative codes found
RIV/00216208:11160/15:10312631 RIV/00179906:_____/15:10312631
Result on the web
<a href="http://www.degruyter.com/view/j/chempap.2015.69.issue-8/chempap-2015-0109/chempap-2015-0109.xml" target="_blank" >http://www.degruyter.com/view/j/chempap.2015.69.issue-8/chempap-2015-0109/chempap-2015-0109.xml</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1515/chempap-2015-0109" target="_blank" >10.1515/chempap-2015-0109</a>

Result language
angličtina
Original language name
Synthesis and antimicrobial activity of sulphamethoxazole-based ureas and imidazolidine-2,4,5-triones
Original language description
Progression of drug resistance among bacterial and fungal pathogens justifies the development of novel antimicrobial agents. Thus, a series of novel sulphamethoxazole-based ureas and imidazolidine-2,4,5-triones have been designed and synthesised. The urea derivatives were obtained by the reaction of sulphamethoxazole and isocyanates, and their cyclisation to imidazolidine-2,4,5-triones was performed via oxalyl chloride. All synthesised derivatives were evaluated in vitro to determine their activity against gram-positive and gram-negative bacteria, fungi, Mycobacterium tuberculosis, and atypical mycobacteria and their cytotoxicity. The growth of mycobacteria was inhibited within the range of 4-1000 mu M and M. tuberculosis was the least-susceptible strain. 4-(3-Heptylureido)-N-(5-methylisoxazol-3-yl)benzenesulphonamide was identified as the most promising compound because it exhibited the highest activity against atypical mycobacteria at minimum inhibitory concentrations, from 4 mu M, a
Czech name
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Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
FR - Pharmacology and apothecary chemistry
OECD FORD branch
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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)

Publication year
2015
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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