Identifikační kód |
RIV/00216208:11160/22:10450828 |
Název v anglickém jazyce |
Comprehensive insight into anti-staphylococcal and anti-enterococcal action of brominated and chlorinated pyrazine-based chalcones |
Druh |
J - Recenzovaný odborný článek (Jimp, Jsc a Jost) |
Poddruh |
J/A - Článek v odborném periodiku je obsažen v databázi Web of Science společností Thomson Reuters s příznakem „Article“, „Review“ nebo „Letter“ (Jimp) |
Jazyk |
eng - angličtina |
Vědní obor |
30104 - Pharmacology and pharmacy |
Rok uplatnění |
2022 |
Kód důvěrnosti údajů |
S - Úplné a pravdivé údaje o výsledku nepodléhající ochraně podle zvláštních právních předpisů. |
Počet výskytů výsledku |
3 |
Popis výsledku v anglickém jazyce |
The greatest threat and medicinal impact within gram-positive pathogens are posed by two bacterial genera, Staphylococcus and Enterococcus. Chalcones have a wide range of biological activities and are recognized as effective templates in medicinal chemistry. This study provides comprehensive insight into the anti-staphylococcal and anti-enterococcal activities of two recently published brominated and chlorinated pyrazine-based chalcones, CH-0y and CH-0w. Their effects against 4 reference and 12 staphylococcal and enterococcal clinical isolates were evaluated. Bactericidal action, the activity in combination with selected conventional antibiotics, the study of post-antimicrobial effect (PAE, PAE/SME), and in vitro and in vivo toxicity, were included. In CH-0y, anti-staphylococcal activity ranging from MIC = 15.625 to 62.5 mu M, and activity against E. faecium from 31.25 to 62.5 mu M was determined. In CH-0w, anti-staphylococcal activity ranging from 31.25 to 125 mu M, and activity against E. faecium and E. faecalis (62.5 mu M) was revealed. Both CH-0y and CH-0w showed bactericidal action, beneficial impact on bacterial growth delay within PAE and PAE/SME studies, and non/low toxicity in vivo. Compared to CH-0w, CH-0y seems to have higher anti-staphylococcal and less toxic potential. In conclusion, chalcones CH-0y and CH-0w could be considered as structural pattern for future adjuvants to selected antibiotic drugs. |
Klíčová slova oddělená středníkem |
post-antimicrobial effect;in vivo toxicity;checkerboard assays;multidrug-resistant enterococci;coagulase-negative staphylococci;methicillin- and vancomycin-resistant Staphylococcus aureus;pyrazine-based chalcones;halogenated chalcones |
Stránka www, na které se nachází výsledek |
https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=3ffYR2OYyx |
DOI výsledku |
10.3389/fmicb.2022.912467 |
Odkaz na údaje z výzkumu |
- |