Novel nucleoside analogues named "triazoxins" were synthesized. Of these, two analogues were found to be highly effective against Giardia lamblia, an intestinal parasite and a major cause of waterborne infection, worldwide. While compound 7 reduced the growth of trophozoites in culture (IC50, ~5 μM), compound 21 blocked the in vitro cyst production (IC50 ~5 μM). Compound 21 was also effective against trophozoites (IC50, ~36 μM). A third analogue (compound 8) was effective against both trophozoites (IC50, ~36 μM) and cysts (IC50, ~20 μM) although at higher concentration. Thus triazoxin analogues are unique and exhibit morphology (i.e., trohozoites or cysts) -specific effects against Giardia.

中文翻译：

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三唑嗪：具有抗贾第鞭毛虫活性的新型核苷。

合成了名为“三唑嗪”的新型核苷类似物。其中，有两种类似物被发现对对抗兰氏贾第鞭毛虫非常有效，兰氏贾第鞭毛虫是一种肠道寄生虫，也是全世界水传播感染的主要原因。化合物 7 减少培养物中滋养体的生长（IC50，~5 μM），而化合物 21 则阻断体外包囊生成（IC50~5 μM）。化合物 21 对滋养体也有效（IC50，~36 μM）。第三种类似物（化合物 8）对滋养体（IC50，~36 μM）和包囊（IC50，~20 μM）均有效，尽管浓度较高。因此，三唑嗪类似物是独特的并且表现出针对贾第鞭毛虫的形态学（即，长孢子或包囊）特异性作用。