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首页> 外文期刊>Journal of Medicinal Chemistry >L-Cystine Diamides as L-Cystine Crystallization Inhibitors for Cystinuria
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L-Cystine Diamides as L-Cystine Crystallization Inhibitors for Cystinuria

机译:L-胱氨酸二酰胺作为胱氨酸尿症的L-胱氨酸结晶抑制剂

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摘要

L-Cystine bismorpholide (la) and L-cystine bis(N'-methylpiperazide) (1b) were seven and twenty-four times more effective than L-cystine dimethyl ester (CDME) in increasing the metastable supersaturation range of L-cystine, respectively, effectively inhibiting L-cystine crystallization. This behavior can be attributed to inhibition of crystal growth at microscopic length scale, as revealed by atomic force microscopy. Both 1a and 1b are more stable than CDME, and 1b was effective in vivo in a knockout mouse model of cystinuria.
机译:L-胱氨酸双吗啉化物(Ia)和L-胱氨酸双(N'-甲基哌嗪)(1b)在增加L-胱氨酸的亚稳态过饱和范围方面比L-胱氨酸二甲基酯(CDME)高7到24倍,分别有效抑制L-胱氨酸的结晶。如原子力显微镜所揭示的,这种行为可以归因于在微观长度尺度上晶体生长的抑制。 1a和1b都比CDME更稳定,并且1b在半胱氨酸尿症的敲除小鼠模型中有效。

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