首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Hypervalent iodine(III) mediated synthesis of novel unsymmetrical 2,5-disubstituted 1,3,4-oxadiazoles as antibacterial and antifungal agents.
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Hypervalent iodine(III) mediated synthesis of novel unsymmetrical 2,5-disubstituted 1,3,4-oxadiazoles as antibacterial and antifungal agents.

机译:高价碘(III)介导的新型不对称2,5-二取代的1,3,4-恶二唑类化合物作为抗菌剂和抗真菌剂。

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摘要

A series of novel 2,5-disubstituted 1,3,4-oxadiazoles 4 have been conveniently synthesized by oxidative cyclization of pyrazolylaldehyde N-acylhydrazones 3 promoted by iodobenzene diacetate under mild conditions (11 examples, up to 92% isolated yields). All the eleven compounds were tested in vitro for their antibacterial activity against gram-positive bacteria namely, Staphylococcus aureus, Bacillus subtilis and two gram-negative bacteria namely, Escherichia coli and Pseudomonas aeruginosa. All the synthesized compounds were also tested for their inhibitory action against two strains of fungus.
机译:通过在温和条件下由碘代苯二乙酸酯促进的吡唑基醛N-酰基hydr三酮3的氧化环化反应,可以方便地合成一系列新颖的2,5-二取代的1,3,4-恶二唑4(11个实例,分离产率高达92%)。在体外测试了所有11种化合物对革兰氏阳性菌,即金黄色葡萄球菌,枯草芽孢杆菌和两种革兰氏阴性菌,即大肠杆菌和铜绿假单胞菌的抗菌活性。还测试了所有合成的化合物对两种菌株的抑制作用。

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