- Synthesis and antimicrobial activities of novel sorbic and benzoic acid amide derivatives
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A series of sorbic and benzoic acid amide derivatives were synthesized by conjugating sorbic acid (SAAD, a1–a7) or benzoic acid (BAAD b1–b6) with amino acid esters and their antimicrobial activities were investigated against Escherichia coli, Bacillus subtilis and Staphylococcus aureus, mixed bacteria from rancid milk, Saccharomyces cerevisiae, and Aspergillus niger. The antimicrobial activity of sorbic acid amides was better than that of benzoic acid amides. The minimum inhibitory concentrations (MIC) of compound isopropyl N-[1-oxo-2, 4-hexadien-1-yl]-L-phenylalaninate (a7) were 0.17 mM against B. subtilis, and 0.50 mM against S. aureus, while the MIC values of sorbic acid were more than 2 mM respectively. Also, compound a7 displayed pH-independent antimicrobial activity in the range of pH 5.0–9.0 and was effective at pH 9.0. These results demonstrated that the conjugation of sorbic acid with amino acid esters led to significant improvement of in vitro antimicrobial attributes, but little effect was observed for benzoic acid amide derivatives.
- Wei, Qingyi,Wang, Xiaomei,Cheng, Jun-Hu,Zeng, Guangxiang,Sun, Da-Wen
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p. 220 - 232
(2018/06/26)
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- Antibacterial preservative is sorbic acid amino ester derivative and its preparation method
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The invention belongs to the field of synthesis of a drug, and relates to a sorbic acid-amino acid ester derivate of an antimicrobial preservative and a preparation method thereof. The preparation method comprises the steps of: enabling amino acid and alcohol to react to generate amino-acid ester by utilizing an acyl chloride method, and then reacting with amino-acid ester by sorbic acid after acylating chlorination, so as to synthesize the amino acid ester derivate of the sorbic acid. The amino acid ester derivate of the novel compound sorbic acid obtained by the method has no sensitization on skin of a human body, is suitable for different pH systems with large ranges, has antibacterial broad-spectrum property and good potential application value, and can be used as the antimicrobial preservative applied to corrosion prevention and antibiosis of foods, drugs, cosmetics, pesticides, leather products and wood materials.
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Paragraph 0042
(2016/11/02)
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- THIAZOLE DERIVATIVES AS SGLT2 INHIBITORS AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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The present invention relates to a novel compound with thiazole ring having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes.
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Page/Page column 59-60
(2012/01/06)
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