2-乙酰基吡啶硫代半卡巴腙对罗德西亚锥虫的体外活性
Activity of 2-acetylpyridine thiosemicarbazones against Trypanosoma rhodesiense in vitro.
作者信息
Casero R A, Klayman D L, Childs G E, Scovill J P, Desjardins R E
出版信息
Antimicrob Agents Chemother. 1980 Aug;18(2):317-22. doi: 10.1128/AAC.18.2.317.
Abstract
Twenty-seven 2-acetylpyridine thiosemicarbazones and analogs were tested for antitrypanosomal activity against Trypanosoma rhodesiense using a semiautomated in vitro assay system. Activity was determined by relative inhibition of uptake of two radiolabeled macromolecular precursors, [methyl-3H]thymidine and L-[U-14C]leucine, as compared to untreated controls. It was observed that the nitrogen atom of the pyridyl moiety of the 2-acetylpyridine thiosemicarbazones was essential for antitrypanosomal activity. The 2-acetylpyridine thiosemicarbazones generally inhibited the uptake of L-[U-14C]leucine to a greater extent than they inhibited [methyl-3H]thymidine uptake. Twenty-four of the 27 compounds tested exhibited activity comparable to that found for the antitrypanosomal agent ethidium bromide.
摘要
使用半自动体外检测系统，对27种2-乙酰基吡啶硫代半卡巴腙及其类似物进行了抗罗德西亚锥虫的抗锥虫活性测试。通过与未处理对照相比，对两种放射性标记的大分子前体[甲基-³H]胸腺嘧啶核苷和L-[U-¹⁴C]亮氨酸摄取的相对抑制来确定活性。观察到2-乙酰基吡啶硫代半卡巴腙吡啶部分的氮原子对于抗锥虫活性至关重要。2-乙酰基吡啶硫代半卡巴腙通常对L-[U-¹⁴C]亮氨酸摄取的抑制程度大于对[甲基-³H]胸腺嘧啶核苷摄取的抑制程度。所测试的27种化合物中有24种表现出与抗锥虫剂溴化乙锭相当的活性。
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