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首页> 外文期刊>Chemical and Pharmaceutical Bulletin >Synthesis and Antimicrobial Evaluation of Some New 1,2-Bis-(2-(N-arylimino)-1,3-thiazolidin-3-yl)ethane Derivatives
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Synthesis and Antimicrobial Evaluation of Some New 1,2-Bis-(2-(N-arylimino)-1,3-thiazolidin-3-yl)ethane Derivatives

机译:一些新型1,2-双-(2-(N-芳基氨基)-1,3-噻唑烷-3-基)乙烷衍生物的合成及抗菌性能评价

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摘要

N,N'-Diarylethylene-bis-thiourea derivatives 1 and 8 were synthesized and their reactions with hydra-zonoyl chlorides yielded the corresponding bis-(2-(N-arylimino)-1,3-thiazolidine derivatives 5a-d and lla-c. The reaction of compound 1 with several a-haloketones afforded the bis-(5-methyl-2-(N-phenylimino)-1,3-thiazolidine derivatives 15a-c and 19a,b. The newly synthesized compounds were tested for their antimicrobial activity against four fungi, two Gram-positive and two Gram-negative bacteria and showed high antibacterial and antifungal activities against all the test microorganisms except Pseudomonas aeruginosa and Candida albicans. Compounds 5b, 15b and 19a exhibited the highest activities against the test microorganisms. The MIC evaluation showed that compound 15b has higher activity than Amphotericin B and Ampicillin against all tested fungi and Gram-positive bacteria (Staphylococcus pneumonia) and showed similar activity like Ampicillin against Gram-negative bacteria (Escherichia coli).
机译:合成了N,N′-二芳基乙烯-双硫脲衍生物1和8,它们与羟基-酰氯的反应产生了相应的双-(2-(N-芳基氨基)-1,3-噻唑烷衍生物5a-d和IIa- c。化合物1与几种α-卤代酮反应,得到双-(5-甲基-2-(N-苯基亚氨基)-1,3-噻唑烷衍生物15a-c和19a,b。测试了新合成的化合物的它们对四种真菌,两种革兰氏阳性细菌和两种革兰氏阴性细菌具有抗菌活性,并且对除铜绿假单胞菌和白色念珠菌以外的所有测试微生物均显示出很高的抗菌和抗真菌活性;化合物5b,15b和19a表现出对测试微生物的最高活性。 MIC评价显示,化合物15b对所有测试的真菌和革兰氏阳性细菌(葡萄球菌)的活性均比两性霉素B和氨苄青霉素高,并且显示出与氨苄西林类似的活性,对所有革兰氏阴性细菌(埃舍里奇大肠杆菌)。

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