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3-(N-甲基)异吲哚酮的2-噻吩甲酰腙和异烟酰腙配合物。它们的抗菌活性研究。

Complexes of 2-thiophenecarbonyl and isonicotinoyl hydrazones of 3-(N-methyl)isatin. A study of their antimicrobial activity.

作者信息

Rodríguez-Argüelles María C, Mosquera-Vázquez Sandra, Tourón-Touceda Patricia, Sanmartín-Matalobos Jesús, García-Deibe Ana M, Belicchi-Ferrari Marisa, Pelosi Giorgio, Pelizzi Corrado, Zani Franca

机构信息

Departamento de Química Inorgánica, Universidade de Vigo, 36200 Vigo, Spain.

出版信息

J Inorg Biochem. 2007 Jan;101(1):138-47. doi: 10.1016/j.jinorgbio.2006.09.004. Epub 2006 Sep 19.

Abstract

Cobalt(II), nickel(II), copper(II) and zinc(II) complexes of 2-thiophenecarbonyl and isonicotinoyl hydrazones of 3-(N-methyl)isatin (HL(1) and HL(2), respectively) were synthesized and characterized, being the crystal structures of HL(1), HL(2) and [Ni(L(1))(2)].2CHCl(3) elucidated by X-ray diffraction techniques. The in vitro antimicrobial activity of all these compounds was tested against several bacteria and fungi. HL(1)and its complexes exhibited a strong inhibition of the growth of Haemophilus influenzae (MIC 0.15-1.50microg/mL) and good antibacterial properties towards Bacillus subtilis (MIC 3-25microg/mL). The minimal inhibitory concentration (MIC) was defined as the lowest concentration of compound inhibiting the growth of each strain. The antibacterial effectiveness was confirmed against a number of Gram positive bacteria, including methicillin-resistant Staphylococcus aureus. Yeasts and moulds showed a low susceptibility, except the dermatophyte mould Epidermophyton floccosum that is inhibited at concentrations ranging from 6 to 50microg/mL. In general, the antimicrobial activity of the thiophene derivatives was greater than that of the isonicotinic analogues.

摘要

合成并表征了3-(N-甲基)异吲哚酮与2-噻吩甲酰腙和异烟酰腙形成的钴(II)、镍(II)、铜(II)和锌(II)配合物(分别为HL(1)和HL(2)),通过X射线衍射技术解析了HL(1)、HL(2)和[Ni(L(1))(2)].2CHCl(3)的晶体结构。测试了所有这些化合物对几种细菌和真菌的体外抗菌活性。HL(1)及其配合物对流感嗜血杆菌的生长表现出强烈抑制作用(MIC为0.15 - 1.50μg/mL),对枯草芽孢杆菌具有良好的抗菌性能(MIC为3 - 25μg/mL)。最低抑菌浓度(MIC)定义为抑制各菌株生长的化合物最低浓度。证实了其对多种革兰氏阳性菌具有抗菌效果,包括耐甲氧西林金黄色葡萄球菌。酵母和霉菌表现出低敏感性,除了絮状表皮癣菌在6至50μg/mL浓度范围内受到抑制。总体而言,噻吩衍生物的抗菌活性大于异烟酸类似物。

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