Functionally substituted 2-aminothiazoles as antimicrobial agents: in vitro and in silico evaluation
2023
Аутори:
Petrou, AnthiKartsev, Victor
Geronikaki, Athina
Glamočlija, Jasmina
Ćirić, Ana
Soković, Marina
Тип документа:
Чланак у часопису (Коригована верзија)
,
© 2023 by Taylor & Francis Group
Метаподаци
Приказ свих података о документуАпстракт:
Nine new functionally substituted derivatives of 2-aminothiazole
were evaluated for antimicrobial activity using microdilution
method against the panel of eight bacterial and eight fungal strains.
Evaluation of antibacterial activity revealed that compounds are
potent antibacterial agents, more active than ampicillin and strep tomycin except of some compounds against B. cereus and En.
cloacae. The best compound appeared to be compound 8. The
most sensitive bacteria appeared to be En. cloacae, while L. mono cytogenes was the most resistant. Compounds also exhibited good
antifungal activity much better than two reference drugs, ketoco nazole and bifonazole. Compound 1 exhibited the best antifungal
activity. The most sensitive fungus was T. viride, while A. fumigatus
was the most resistant. Bacteria as well as fungi in general showed
different sensitivity towards compounds tested. Molecular docking
studies revealed that MurB inhibition is probably involved in the
mechanism of antibacterial activity, while CYP51 of C. albicans is
responsible for the mechanism of antifungal activity. Finally, it
should be mentioned that all compounds displayed very good
druglikeness scores
Кључне речи:
PASS; antibacterial; antifungal; docking studies; MurB; CYP51Извор:
SAR and QSAR in Environmental Research, 2023, 34, 5, 359-414Финансирање / пројекти:
- Министарство науке, технолошког развоја и иновација Републике Србије, институционално финансирање - 200007 (Универзитет у Београду, Институт за биолошка истраживања 'Синиша Станковић') (RS-MESTD-inst-2020-200007)