[Antimicrobial activity of selected aqua-carboxyl-cupric complexes].

Ceskoslovenska farmacie Pub Date : 1992-03-01
J Sokolík, M Blahová, B Lucanská, D Mlynarcík, A Valent, L Andrezälová, O Svajlenová, M Zemlicka
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Abstract

The activity of compounds of different structural types of aqua-complexes of the composition Cu(R-COO)2.nH2O-methoxybenzoatocupric complexes, R = 2-, 3- and 4-methoxyphenyl (n = 1, 1 and 3); aryloxyacetatocupric complexes, R = phenoxymethyl (n = 3), 2-, 3- and 4-chlorophenoxymethyl (n = 4, 2 and 2) and 1-naphthoxymethyl (n = 4), and furthermore isomeric furanecarboxylato-(R = 2- or 3-furyl, n = 3, or 1) and thiophencarboxylatocupric complexes (R = 2- or 3-thienyl, n = 1 and 1), was examined by the methods of the 1st screening on selected anthropo- and phytopathogenic microorganisms. The effects of all aqua-complexes (suspension dosage form) on the representatives of bacteria and yeasts are minimal. On the other hand, the effect of these substances on the causative agents of dermatomycoses (Trichophyton terrestre, Microsporum gypseum) in the case of methoxybenzoato- and furoatocupric complexes achieves a MIC value of 500 micrograms/cm3 and lower. The activity against phytopathogenic fungi (both in vitro and in vivo experiments) is generally relatively low at 0.05% concentration of active ingredients (dispersible powders). At the same time the antimicrobial activity of the pertinent free carboxylic acids was investigated in relation to the cupric salts being formed. They are able to form the required pharmacoactive form prevalently as late as they are in the form of aqua-carboxylatocupric complexes.

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[选定的水-羧基-铜配合物的抗菌活性]。
不同结构类型的Cu(R-COO)2水络合物的活性。nh20 -甲氧基苯甲酸三铜配合物,R = 2-、3-和4-甲氧基苯基(n = 1,1和3);采用第一次筛选的方法,在选定的人病原微生物和植物病原微生物上检测了芳氧乙酸二铜配合物R =苯氧甲基(n = 3)、2-、3-和4-氯苯氧甲基(n = 4、2和2)和1-萘氧甲基(n = 4),以及异构体呋喃甲氧基-(R = 2或3-呋喃基,n = 3或1)和硫氧甲氧基配合物R = 2或3-噻吩基,n = 1和1)。所有的水络合物(悬浮液剂型)对细菌和酵母的代表的影响是最小的。另一方面,在甲氧基苯甲酸和呋喃三铜配合物的情况下,这些物质对皮肤真菌(地毛菌,石膏小孢子菌)病原体的影响达到了500微克/立方厘米或更低的MIC值。在0.05%的活性成分(分散粉末)浓度下,对植物病原真菌的活性(体外和体内实验)通常相对较低。同时研究了相关游离羧酸的抑菌活性与所形成的铜盐的关系。他们能够形成所需的药物活性形式,普遍晚,因为他们的形式是水-羧酸铜络合物。
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