Abstract:
:A series of amides derived from vanillic acid were obtained by coupling reactions using PyBOP ((Benzotriazol-1-yloxy)tripyrrolidinophosphonium hexafluorophosphate) and DCC (Dicyclohexylcarbodiimide) coupling reagents. These were submitted to biological evaluation for species of Candida, Staphylococcus, and Pseudomonas. The microdilution method in broth was used for the antimicrobial testing to determine the Minimum Inhibitory Concentration (MIC) and to verify the likely mechanism of action for antifungal activity. The ten amides were obtained with yields ranging from 28.81 to 86.44%, and three compounds were novel. In the antibacterial evaluation, the amides (in their greatest concentrations) were bioactive against Staphylococcus aureus strain ATCC 25925. Meanwhile, all of the tested amides presented antifungal activity against at least one strain. The amide with best antifungal profile was compound 7, which featured an MIC of 0.46 μmol/mL, and a mechanism of action involving the plasma membrane and fungal cell wall. The presence of a methyl group in the para position of the aromatic ring is suggested which enhances the activity of the compound against fungi. Docking studies of the ten compounds using the protein 14α-demethylase as a biological target were also performed. The biological results presented good correlation with molecular docking studies demonstrating that a possible site of antifungal action for bioactive amides is the enzyme 14α-demethylase.
journal_name
Biomed Res Intjournal_title
BioMed research internationalauthors
Santos Oliveira AJM,de Castro RD,Pessôa HLF,Wadood A,de Sousa DPdoi
10.1155/2019/9209676subject
Has Abstractpub_date
2019-04-15 00:00:00pages
9209676eissn
2314-6133issn
2314-6141journal_volume
2019pub_type
杂志文章abstract::The purpose of this study is to evaluate the therapeutic effects of human umbilical cord-derived mesenchymal stem cells (hUC-MSC) activated by curcumin (CUR) on PC12 cells induced by 1-methyl-4-phenylpyridinium ion (MPP+), a cell model of Parkinson's disease (PD). The supernatant of hUC-MSC and hUC-MSC activated by 5 ...
journal_title:BioMed research international
pub_type: 杂志文章
doi:10.1155/2016/9140541
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journal_title:BioMed research international
pub_type: 杂志文章
doi:10.1155/2018/1742326
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abstract::Non-small-cell lung cancer (NSCLC) patients often develop bone metastases (BM), and the overall survival for these patients is usually perishing. However, a model with high accuracy for predicting the survival of NSCLC with BM is still lacking. Here, we aimed to establish a model based on artificial intelligence for p...
journal_title:BioMed research international
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abstract::Hepatitis B virus (HBV) infection is the predominant risk factor for chronic hepatitis B (CHB). The association between HBV infection and human leukocyte antigen- (HLA-) DQ polymorphism (rs2856718 and rs7453920) has been demonstrated in other studies; however, the results were controversial or inconclusive. Therefore,...
journal_title:BioMed research international
pub_type: 杂志文章,meta分析
doi:10.1155/2017/9679843
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journal_title:BioMed research international
pub_type: 杂志文章,meta分析,评审
doi:10.1155/2016/8034613
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journal_title:BioMed research international
pub_type: 杂志文章,评审
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journal_title:BioMed research international
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journal_title:BioMed research international
pub_type: 杂志文章,评审
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journal_title:BioMed research international
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journal_title:BioMed research international
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journal_title:BioMed research international
pub_type: 杂志文章
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journal_title:BioMed research international
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journal_title:BioMed research international
pub_type: 临床试验,杂志文章
doi:10.1155/2020/7131590
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journal_title:BioMed research international
pub_type: 杂志文章
doi:10.1155/2015/615034
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journal_title:BioMed research international
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doi:10.1155/2018/9594568
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pub_type: 杂志文章
doi:10.1155/2019/4370382
更新日期:2019-10-07 00:00:00
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journal_title:BioMed research international
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更新日期:2019-01-06 00:00:00
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pub_type: 杂志文章
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journal_title:BioMed research international
pub_type: 杂志文章,已发布勘误
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journal_title:BioMed research international
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journal_title:BioMed research international
pub_type: 杂志文章
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更新日期:2015-01-01 00:00:00