期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 123, 期 -, 页码 532-543出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.07.074
关键词
Antibacterial; Antifungal; Antioxidant activity; Cytotoxic effects; D-glucose; Isatins; Microwave-assisted synthesis; Methicillin-resistant Staphylococcus aureus; Thiosemicarbazones
Some new isatin N-(2,3,4,6-tetra-O-acetyl-beta-D-glucopyranosyl)thiosemicarbazones 4a-t with different substituents at 1-, 5- and 7-positions of isatin ring have been synthesized by reaction of N-(2,3,4,6-tetra-O-acetyl-beta-D-glucopyranosyl)thiosemicarbazide 2 with corresponding isatins 3a-t. Compounds 4a-t were evaluated in vivo for antioxidant activity and in vitro for anti-microorganism activities. The MIC values were found for Gram positive bacteria (MIC = 1.56-6.25 mu M), for Gram negative bacteria (MIC = 12.5 mu M), and for fungi Aspergillus niger (MIC = 3.12-12.5 mu M), Fusarium oxysporum (MIC = 6.25-12.5 mu M) and Saccharomyces cerevisiae (MIC = 6.25-12.5 mu M). Regarding the antioxidant activity, the SOD, GHS-Px and catalase activities of 4c-i and 4m-r were MIC = 10.57-10.85, 0.27-0.93 and 345.45-399.75 unit/mg protein, respectively. Compounds 4e-h had MIC values of 0.78, 1.56, and 3.12 mu M for three clinical MRSA isolates. Compound 4e showed the selective cytotoxic effects against some cancer (LU-1, HepG2, MCF7, P338, SW480, KB) cell lines and normal fibroblast cell line NIH/3T3. (C) 2016 Elsevier Masson SAS. All rights reserved.
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