New N-(oxazolylmethyl)-thiazolidinedione Active against Candida albicans Biofilm: Potential Als Proteins Inhibitors
| Autor: | Mariana Carmen Chifiriuc, Gabriel Marc, Luminița Măruțescu, Mihaela Duma, Smaranda Oniga, Adrian Pîrnău, Laurian Vlase, Ovidiu Oniga, Cătălin Araniciu |
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| Jazyk: | angličtina |
| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
thiazolidine-2 4-dione Pharmaceutical Science Virulence Context (language use) Article biofilm Analytical Chemistry Microbiology lcsh:QD241-441 Fungal Proteins 03 medical and health sciences Antibiotic resistance lcsh:Organic chemistry Drug Discovery Candida albicans invasins Cell Adhesion Humans Physical and Theoretical Chemistry biology Chemistry Organic Chemistry oxazole Biofilm Antimicrobial biology.organism_classification Corpus albicans adhesion 030104 developmental biology Chemistry (miscellaneous) Biofilms Molecular Medicine Thiazolidinediones Als Bacteria |
| Zdroj: | Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry Molecules, Vol 23, Iss 10, p 2522 (2018) Molecules Volume 23 Issue 10 |
| ISSN: | 1420-3049 |
| Popis: | C. albicans is the most frequently occurring fungal pathogen, and is becoming an increasing public health problem, especially in the context of increased microbial resistance. This opportunistic pathogen is characterized by a versatility explained mainly by its ability to form complex biofilm structures that lead to enhanced virulence and antibiotic resistance. In this context, a review of the known C. albicans biofilm formation inhibitors were performed and a new N-(oxazolylmethyl)-thiazolidinedione scaffold was constructed. 16 new compounds were synthesized and characterized in order to confirm their proposed structures. A general antimicrobial screening against Gram-positive and Gram-negative bacteria, as well as fungi, was performed and revealed that the compounds do not have direct antimicrobial activity. The anti-biofilm activity evaluation confirmed the compounds act as selective inhibitors of C. albicans biofilm formation. In an effort to substantiate this biologic profile, we used in silico investigations which suggest that the compounds could act by binding, and thus obstructing the functions of, the C. albicans Als surface proteins, especially Als1, Als3, Als5 and Als6. Considering the well documented role of Als1 and Als3 in biofilm formation, our new class of compounds that target these proteins could represent a new approach in C. albicans infection prevention and management. |
| Databáze: | OpenAIRE |
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