ANTIFUNGAL AND ANTITUMOR-ACTIVITY OF HETEROCYCLIC THIOSEMICARBAZONES AND THEIR METAL-COMPLEXES - CURRENT STATUS
ANTIFUNGAL AND ANTITUMOR-ACTIVITY OF HETEROCYCLIC THIOSEMICARBAZONES AND THEIR METAL-COMPLEXES - CURRENT STATUS
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DOI：
10.1007/bf01062223
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发表时间：
1992-06-01
期刊：
影响因子：
3.5
通讯作者：
WEST, DX
中科院分区：
文献类型：
--
作者：
LIBERTA, AE;WEST, DX
已测定了75种以上取代的缩氨基硫脲及其金属配合物的抗真菌活性。它们的活性受连接在缩氨基硫脲部分的1 N和4 N处的取代基团的显著影响。2-取代吡啶缩氨基硫脲的活性最高，2-甲酰基吡啶、2-乙酰基吡啶和2-苯甲酰基吡啶衍生物及其金属配合物的活性也不同。此外，4 N-烷基-、4 N-芳基-、4 N-二烷基-和3-氮杂环缩氨基硫脲及其金属络合物的活性存在差异，并且这些亚组中的每一个之间的取代基大小也存在变化。Cu（II）络合物通常比未络合的缩氨基硫脲更有活性，后者在许多情况下显示出与Ni（II）络合物相似的活性。在Cu（II）络合物中的缩氨基硫脲配体的还原电位、配体场的强度和各种光谱性质可以与抑制活性相关。
More than 75 substituted thiosemicarbazones and a number of metal complexes of each have been assayed for their antifungal activity. Their activity is significantly affected by the substituted groups attached at both 1N and 4N of the thiosemicarbazone moiety. Greatest activity occurs for 2-substituted pyridine thiosemicarbazones with differences observed for 2-formylpyridine, 2-acetylpyridine and 2-benzoylpyridine derivatives and their metal complexes. Further, there are activity differences for 4N-alkyl-, 4N-aryl-, 4N-dialkyl- and 3-azacyclothiosemicarbazones and their metal complexes as well as changes in the substituent size among each of these subgroups. Cu(II) complexes are often more active than the uncomplexed thiosemicarbazones, with the latter showing similar activity to Ni(II) complexes in many instances. The reduction potential of the thiosemicarbazone ligand in a Cu(II) complex, the strength of the ligand field and various spectral properties can be correlated to the inhibitory activity.