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Peptide dendrimers as antifungal agents and carriers for potential antifungal agent-N3 -(4-methoxyfumaroyl)-(S)-2,3-diaminopropanoic acid-synthesis and antimicrobial activity.
Journal of Peptide Science ( IF 1.8 ) Pub Date : 2019-12-16 , DOI: 10.1002/psc.3226
Magdalena Stolarska 1 , Katarzyna Gucwa 2 , Zofia Urbańczyk-Lipkowska 3 , Ryszard Andruszkiewicz 2
Affiliation  

A series of peptide dendrimers and their conjugates with antimicrobial agent FMDP (N3‐(4‐methoxyfumaroyl)‐(S)‐2,3‐diamino‐propanoic acid) were synthesized. The obtained compounds were tested for the antibacterial and antifungal activity. All novel dendrimers displayed much better activity against the tested strains than FMDP itself. Moreover, their conjugates with FMDP also exhibited antimicrobial activity. The most promising molecules were tested against a broad selection of fungal strains. The analysis of their antifungal properties indicates that the examined molecules are efficient growth inhibitors of fluconazole‐resistant hospital‐acquired strains. Moreover, an application of amphiphilic branched peptides such as FMDP carriers suggests that transport mechanism involves more likely the cell membrane perturbation than the mediation of the specific transport proteins. The activity of obtained compounds strongly depends on the specific structure of the molecule.

中文翻译:

肽树状聚合物作为抗真菌剂和载体,用于潜在的抗真菌剂-N3-(4-甲氧基富马酰基)-(S)-2,3-二氨基丙酸的合成和抗菌活性。

一系列肽树状大分子及其与抗菌剂FMDP(N 3-(4-甲氧基富马酰基)-(S)-2,3-二氨基丙酸)。测试获得的化合物的抗菌和抗真菌活性。与FMDP本身相比,所有新的树状聚合物对被测菌株均显示出更好的活性。而且,它们与FMDP的缀合物也显示出抗菌活性。测试了最有前途的分子针对多种真菌菌株的测试。对它们的抗真菌特性的分析表明,所检查的分子是耐氟康唑的医院获得菌株的有效生长抑制剂。此外,两亲性分支肽(如FMDP载体)的应用表明,与特定转运蛋白的介导相比,转运机制更可能涉及细胞膜的扰动。
更新日期:2019-12-16
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