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Design and Synthesis of Novel 1,3-Thiazole and 2-Hydrazinyl-1,3-Thiazole Derivatives as Anti-Candida Agents: In Vitro Antifungal Screening, Molecular Docking Study, and Spectroscopic Investigation of their Binding Interaction with Bovine Serum Albumin
| Content Provider | Semantic Scholar |
|---|---|
| Author | Pricopie, Andreea-Iulia Ionuț, Ioana Marc, Gabriel Arseniu, Anca-Maria Vlase, Laurian Grozav, Adriana Gaina, Luiza Vodnar, Dan Cristian Pîrnǎu, Adrian Tiperciuc, Brîndușa Oniga, Ovidiu |
| Copyright Year | 2019 |
| Abstract | In the context of there being a limited number of clinically approved drugs for the treatment of Candida sp.-based infections, along with the rapid development of resistance to the existing antifungals, two novel series of 4-phenyl-1,3-thiazole and 2-hydrazinyl-4-phenyl-1,3-thiazole derivatives were synthesized and tested in vitro for their anti-Candida potential. Two compounds (7a and 7e) showed promising inhibitory activity against the pathogenic C. albicans strain, exhibiting substantially lower MIC values (7.81 μg/mL and 3.9 μg/mL, respectively) as compared with the reference drug fluconazole (15.62 μg/mL). Their anti-Candida activity is also supported by molecular docking studies, using the fungal lanosterol C14α-demethylase as the target enzyme. The interaction of the most biologically active synthesized compound 7e with bovine serum albumin was investigated through fluorescence spectroscopy, and the obtained data suggested that this molecule might efficiently bind carrier proteins in vivo in order to reach the target site. |
| File Format | PDF HTM / HTML |
| PubMed reference number | 31546673 |
| Journal | Medline |
| Volume Number | 24 |
| Alternate Webpage(s) | https://res.mdpi.com/d_attachment/molecules/molecules-24-03435/article_deploy/molecules-24-03435.pdf |
| Alternate Webpage(s) | https://doi.org/10.3390/molecules24193435 |
| Journal | Molecules |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |
