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阴道毛滴虫 AdoHcy 水解酶:5’-修饰腺苷类似物及相关 6-N-环丙基衍生物的作用研究。

AdoHcy hydrolase of Trichomonas vaginalis: studies of the effects of 5'-modified adenosine analogues and related 6-N-cyclopropyl derivatives.

机构信息

Department of Biological Sciences, University of the Pacific, Stockton, CA 95211, USA.

出版信息

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7466-8. doi: 10.1016/j.bmcl.2010.10.014. Epub 2010 Oct 31.

Abstract

Trypanosoma brucei and Trichomonas vaginalis are both parasitic protozoans that are known to share many similar biochemical pathways. Aristeromycin, as well as 5'-iodovinyl and 5'-oxime analogues of adenosine, are potent inhibitors of AdoHcy hydrolase in T. brucei, an enzyme that catalyses the hydrolysis of AdoHcy to adenosine and L-homocysteine. To help determine the role of this enzyme in T. vaginalis, we have tested a library of 5'-modified adenosine derivatives, including 5'-deoxy-5'-(iodomethylene)-adenosine and related 6-N-cyclopropyl analogues. Our results indicate that these inhibitors are effective at inhibiting the growth of T. vaginalis, by as much as 95%.

摘要

布氏锥虫和阴道毛滴虫都是寄生的原生动物,已知它们有许多相似的生化途径。阿利斯特霉素以及腺苷的 5'-碘代乙烯基和 5'-肟类似物是布氏锥虫中 AdoHcy 水解酶的有效抑制剂,该酶催化 AdoHcy 水解为腺苷和 L-高半胱氨酸。为了帮助确定该酶在阴道毛滴虫中的作用,我们测试了包括 5'-脱氧-5'-(碘代亚甲基)-腺苷和相关的 6-N-环丙基类似物在内的 5'-修饰腺苷衍生物文库。我们的结果表明,这些抑制剂能有效抑制阴道毛滴虫的生长,抑制率高达 95%。

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