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一些新型2,3-二甲氧基-3-羟基-2-(1-苯基-3-芳基-4-吡唑基)色满酮的合成与抗菌活性

Synthesis and antibacterial activity of some new 2,3-dimethoxy-3-hydroxy-2-(1-phenyl-3-aryl-4-pyrazolyl)chromanones.

作者信息

Prakash Om, Kumar Rajesh, Sehrawat Rakesh

机构信息

Department of Chemistry, Kurukshetra University, Kurukshetra 136 119, India.

出版信息

Eur J Med Chem. 2009 Apr;44(4):1763-7. doi: 10.1016/j.ejmech.2008.03.028. Epub 2008 Apr 4.

Abstract

Seven new 2,3-dimethoxy-3-hydroxy-2-(1-phenyl-3-aryl-4-pyrazolyl)chromanones (5) have been synthesized by the oxidation of 3-hydroxy-2-(1-phenyl-3-aryl-4-pyrazolyl)chromones (4) with iodobenzene diacetate in methanol. The structures of compounds 5 were established by the combined use of (1)H NMR, IR and mass spectra. All the seven compounds (5) were tested in vitro for their antibacterial activity against gram-positive bacteria namely, Staphylococcus aureus, Staphylococcus epidermidis and Bacillus pumilus and two gram-negative bacteria namely, Salmonella typhi and Pseudomonas aeruginosa. Three compounds, 5d, 5f and 5g, have displayed antibacterial activity comparable to the commercial antibiotics, Linezolid, Cefaclor and Cefuroxime axetial.

摘要

通过在甲醇中用二醋酸碘苯氧化3-羟基-2-(1-苯基-3-芳基-4-吡唑基)色酮(4),合成了七种新的2,3-二甲氧基-3-羟基-2-(1-苯基-3-芳基-4-吡唑基)色满酮(5)。通过结合使用¹H NMR、IR和质谱确定了化合物5的结构。对所有七种化合物(5)进行了体外测试,以检测它们对革兰氏阳性菌金黄色葡萄球菌、表皮葡萄球菌和短小芽孢杆菌以及两种革兰氏阴性菌伤寒沙门氏菌和铜绿假单胞菌的抗菌活性。三种化合物5d、5f和5g表现出与市售抗生素利奈唑胺、头孢克洛和头孢呋辛酯相当的抗菌活性。

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