[Biological effects of coordination compounds of transitional metals. The beta-lactamase inhibitory effect of cis-platin, 2-aminopyridine palladium chloride, clavulanic acid and penicillanic acid sulfonate CP 45,899 in the nitrocefin test and Titertek/microtiter automatic system].

W F Fleck, B Heyn, H P Schröer
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引用次数: 1

Abstract

The beta-lactamase-inhibiting activity of 6m-ethyl-pyrid-2-yl-ammine palladium-dichloride (Pd 25681) and cis-dichloro-diammine-platinum(II) was studied and compared with the enzyme inhibitory action of potassium clavulanate and the penicillanic acid sulfone CP 45899. Using the nitrocefin test method and the Titertek/Microtiter equipment CP 45899 and potassium clavulanate were the strongest inhibitors of the Bacillus cereus beta-lactamase. Cis-dichloro-diammine-platinum(II) was fourfold less active than the palladium complex PD 25681 in äquimolar concentration. The following ID50 values were found: CP 45899: 0.0281 microgram; K-clavulanate: 0.1274 microgram; Pd 25681: 3.8603 microgram; cis-dichlorodiammine-platinum(II): 12.5120 microgram/100 microliter.

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过渡金属配位化合物的生物学效应。顺铂、2-氨基吡啶氯化钯、克拉维酸和青霉酸磺酸盐CP 45,899在硝基芬试验和Titertek/微滴度自动系统中的β -内酰胺酶抑制作用。
研究了6 - m-乙基吡啶-2-基胺二氯化钯(Pd 25681)和顺式二氯二胺铂(II)的β -内酰胺酶抑制活性,并与克拉维酸钾和青霉酸砜CP 45899的酶抑制作用进行了比较。采用硝基芬法和Titertek/Microtiter设备测定,CP 45899和克拉维酸钾是蜡样芽孢杆菌β -内酰胺酶的最强抑制剂。顺式二氯二胺铂(II)在äquimolar浓度下的活性比钯配合物PD 25681低4倍。发现以下ID50值:CP 45899: 0.0281微克;k -克拉维酸:0.1274微克;Pd 25681: 3.8603微克;顺式二氯二胺铂(II): 12.5120微克/100微升。
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