Synthesis and biological activities of new Mannich bases of chlorokojic acid derivatives

Synthesis and biological activities of new Mannich bases of chlorokojic acid derivatives
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DOI:
10.1007/s00044-010-9338-x
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发表时间:
2011-05
影响因子:
2.6
通讯作者:
M. Aytemi̇r;B. Özçelik
M. Aytemi̇r;B. Özçelik
中科院分区:
医学4区
文献类型:
--
作者:
M. Aytemi̇r;B. Özçelik

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合成了一系列新型 6-氯甲基-3-羟基-2-取代的 4H-吡喃-4-酮衍生物,并测试了其体外抗菌、抗真菌和抗病毒特性。从活性结果来看,化合物8-11(MIC:8μg/ml)对金黄色葡萄球菌和粪肠球菌的活性更显着。化合物 1-7 对白色念珠菌和近平滑念珠菌具有高度活性,MIC 值为 8 μg/ml。带有3-氯苯基部分的化合物9被确定为针对RNA病毒PI-3最有活性的化合物。
A novel series of 6-chloromethyl-3-hydroxy-2-substituted 4H-pyran-4-one derivatives were synthesized and tested for their antibacterial, antifungal and antiviral in vitro properties. In the view of activity results, compounds8–11(MIC: 8 μg/ml) were more remarkably active againstStaphylococcus aureusandEnterococcus faecalis. Compounds1–7were highly active againstCandida albicansandC.parapsilosiswith MIC value of 8 μg/ml. Compound9bearing 3-chlorophenyl moiety was determined to be the most active compound against RNA virusPI-3.