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带有N-(3-苯丙基)取代基的多胺是有效的锥虫硫醇还原酶竞争性抑制剂和杀锥虫剂。

Polyamines with N-(3-phenylpropyl) substituents are effective competitive inhibitors of trypanothione reductase and trypanocidal agents.

作者信息

Li Z, Fennie M W, Ganem B, Hancock M T, Kobaslija M, Rattendi D, Bacchi C J, O'Sullivan M C

机构信息

Department of Chemistry, Indiana State University, Terre Haute 47809, USA.

出版信息

Bioorg Med Chem Lett. 2001 Jan 22;11(2):251-4. doi: 10.1016/s0960-894x(00)00643-0.

Abstract

Several N-(3-phenylpropyl)-substituted spermidine and spermine derivatives were prepared and found to be potent competitive inhibitors of Trypanosoma cruzi trypanothione reductase (seven compounds with Ki values < 5 microM are described). The most effective inhibitor studied was compound 12 with a Ki value of 0.151 microM. Six of the compounds described are also effective trypanocides with IC50 values < 1 microM.

摘要

制备了几种N-(3-苯基丙基)取代的亚精胺和精胺衍生物,发现它们是克氏锥虫锥虫硫醇还原酶的有效竞争性抑制剂(描述了7种Ki值<5 microM的化合物)。所研究的最有效抑制剂是化合物12,其Ki值为0.151 microM。所描述的化合物中有6种也是有效的杀锥虫剂,IC50值<1 microM。

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