BIOLOGICAL ACTIONS OF 1,10-PHENANTHROLINE AND 2,2'-BIPYRIDINE HYDROCHLORIDES QUATERNARY SALTS AND METAL CHELATES AND RELATED COMPOUNDS .1. BACTERIOSTATIC ACTION ON SELECTED GRAM-POSITIVE GRAM-NEGATIVE AND ACID-FAST BACTERIA
BIOLOGICAL ACTIONS OF 1,10-PHENANTHROLINE AND 2,2'-BIPYRIDINE HYDROCHLORIDES QUATERNARY SALTS AND METAL CHELATES AND RELATED COMPOUNDS .1. BACTERIOSTATIC ACTION ON SELECTED GRAM-POSITIVE GRAM-NEGATIVE AND ACID-FAST BACTERIA
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DOI：
10.1038/icb.1969.21
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发表时间：
1969-01-01
期刊：
影响因子：
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通讯作者：
DIXSON, S
中科院分区：
文献类型：
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作者：
DWYER, FP;REID, IK;DIXSON, S
报道了稳定、惰性、配位饱和的取代1.10-菲咯啉和2，2 ′-联吡啶碱的Ru（II）螯合物的抑菌活性，以及Ni（II）、Fe（II）、Co（II）、Cu（II）、Zn（II）、Cd（II）和Mn（II）的相应螯合物的抑菌活性。碱和其他化合物的盐酸盐和季盐;主要试验生物，按一般敏感性递减的顺序排列。是M。结核，葡萄球菌。金黄色葡萄球菌、链球菌pneumoniae，Cl.产气荚膜梭菌E.科兰角Ru（II）螯合物的活性组分是作为整体的阳离子，其只能通过弱库仑力和短程力以及可能通过干扰生物氧化还原反应来发挥抗菌作用。然而，不稳定或稳定性低的金属螯合物可能通过其他机制起作用，金属螯合物通常比相应的碱盐酸盐和季盐和邻菲咯啉衍生物的活性比相应的联吡啶高。虽然Ru（II）5-NO2 - 1，10-菲咯啉螯合物的活性远低于其他7种过渡金属的突出抗结核螯合物，但本方法在仅金属离子不同的螯合物之间检测到抑菌活性的其他差异很少。由于每种类型的化合物的逐步甲基化通常增加抗菌活性，渗透或积累在重要部位是最有可能的重要因素，在确定activity.While在临床上有用的局部抗菌药物，选定的化合物给药时，肠胃外被发现是chemotherapeutically无效对实验感染由于葡萄球菌。金黄色葡萄球菌、链球菌肺炎菌M.对选定的金属螯合物的显著的微生物抗性似乎没有发展。
The bacteriostatic activities of stable, inert, coordinately‐saturated Ru(II) chelates of substituted 1.10‐phenanthroline and 2,2′‐bipyridine bases are reported together with those of the corresponding chelates of Ni(II), Fe(II), Co(II), Cu(II), Zn(II), Cd(II) and Mn(II). the hydrochlorides and quaternary salts of the bases and miscellaneous compounds; the principal test organisms, in order of decreasing general seasitivity. wereM. tuberculosis, Staph. aureus, Strep. pneumoniae, Cl. perfringens, E. collandPr. culgaris.The active component of the Ru(II) chelates is the cation as a whole which can only exert antibacterial action by weak Coulombic and short‐range forces and possibly by interference in biological redox reactions. However, metal chelates which are labile or have low stability may act by other mechanisms.Metal chelates generally were more active than corresponding base hydrochlorides and quaternary salts and phenanthroline derivates more active than the corresponding bipyridines. While the Ru(II) chelatc of 5‐NO2‐ 1,10‐phenanthroline was much less active than the outstandingly antitubercular chelates of the other seven transition metals, few other differences in bacteriostatic activity were detected by the present method between chelates differing only in the metal ion. Since progressive methylation of each type of compound generally increased antibacterial activity, penetration to or accumulation at vital sites are most likely important factors in determining activity.While useful clinically as topical antimicrobials, selected compounds when administered parenterally were found to be chemotherapeutically ineffective against experimental infection due toStaph. aureus, Strep. pneumoniaeorM. tuberculosis.Significant microbial resistance to selected metal chelates does not appear to develop.