2018
DOI: 10.1016/j.ejmech.2017.11.094
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Synthesis and antimicrobial activity of amino acid and peptide derivatives of mycophenolic acid

Abstract: The series of 16 novel amino acid and peptide mycophenolic acid (MPA) derivatives was obtained as potential antibacterial agents. Coupling of MPA with respective amines was optimized with condensing reagents such as EDCI/DMAP and T3P/TEA. Amino acid analogs were received both as methyl esters and also with the free carboxylic group. The biological activity of the products was tested on five references bacterial strains: Klebsiella pneumoniae ATCC 700603 (ESBL), Escherichia coli ATCC 8739, Pseudomonas aeruginos… Show more

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Cited by 25 publications
(14 citation statements)
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“…The mixture was stirred for 2 h in ice bath, and HO‐PCL‐OH of M n = 4.5 × 10 4 (4 g, 8.9 × 10 −5 mol) dissolved in tetrahydrofuran (25 mL) was added. The reaction continued for 24 h at room temperature . The products were precipitated and washed with distilled water for five times and freeze‐dried to give the end‐group heparinized PCL (PCL‐O‐Hep).…”
Section: Methodsmentioning
confidence: 99%
“…The mixture was stirred for 2 h in ice bath, and HO‐PCL‐OH of M n = 4.5 × 10 4 (4 g, 8.9 × 10 −5 mol) dissolved in tetrahydrofuran (25 mL) was added. The reaction continued for 24 h at room temperature . The products were precipitated and washed with distilled water for five times and freeze‐dried to give the end‐group heparinized PCL (PCL‐O‐Hep).…”
Section: Methodsmentioning
confidence: 99%
“…Compounds 125 (SI = 2871.4) , 126 (SI = 33,787.9), and 127 (SI = 7166.7) exhibited higher potency than MPA in vitro . In addition, Siebert et al ( 2018 ) obtained novel amino acid MPA derivatives as potential antibacterial agents. Peptide derivatives proved to be the most versatile, and their strains were relative to most MIC values lower than MPA.…”
Section: Application Of Amino Acids In the Structural Modification Of Natural Productsmentioning
confidence: 99%
“…Similarly, 37.2% of the mycotoxin content in 89 blue‐veined cheese contained quantifiable amounts of mycophenolic acid (Fontaine et al., 2015). Mycophenolic acid was identified as a potent antibiotic against Bacillus anthracis , which was later reported to have antiviral, antifungal, antitumor, and immunosuppressant properties (Siebert, Wysocka, Krawczyk, Cholewiński, & Rachoń, 2018). Selection and use of beneficial fungal strains that enhance the technological and functional properties of cheese and inhibit the growth of toxin‐producing molds can decrease incidences of cheese spoilage while increasing the bioactive property of the cheese product.…”
Section: Microorganisms Associated With Cheese Productionmentioning
confidence: 99%