Oke J M, Watt R A
London School of Pharmacy, University of London.
Afr J Med Med Sci. 1998 Sep-Dec;27(3-4):225-8.
Onchocerciasis is a disease that engages the attention of most researchers. Presently, there is not an ideal onchocerciatic agent, hence the search must continues. Consequently alpha, alpha-trehalose-6-phosphate was synthesised and assessed for onchocerciatic activity against O. volvulus; using diethylcarbamizine citrate as the control drug. Results from this study showed that alpha, alpha-trehalose-6-phosphate is a glucose analogue with effective micro and macro-filaricidal agent, better than that of the control drug. The inhibitory action of this compound on enzyme trehalase is a postulate for the mechanism of action of trehalose-6-phosphate. The structure-activity relationship of this new compound is fully discussed. This study postulates that this compound could be used to eradicate onchocerciasis both in man and animals.
盘尾丝虫病是一种吸引了大多数研究人员关注的疾病。目前，还没有理想的抗盘尾丝虫病药物，因此必须继续进行探索。于是合成了α,α-海藻糖-6-磷酸，并评估其对旋盘尾丝虫的抗盘尾丝虫病活性；使用枸橼酸乙胺嗪作为对照药物。这项研究的结果表明，α,α-海藻糖-6-磷酸是一种葡萄糖类似物，是有效的微丝蚴和成虫杀灭剂，比对照药物效果更好。该化合物对海藻糖酶的抑制作用是海藻糖-6-磷酸作用机制的一种假设。充分讨论了这种新化合物的构效关系。这项研究推测，这种化合物可用于根除人和动物的盘尾丝虫病。
