l-Cystine Diamides as l-Cystine Crystallization Inhibitors for Cystinuria

详细信息    查看全文

• 作者：Longqin Hu ; Yanhui Yang ; Herve Aloysius ; Haifa Albanyan ; Min Yang ; Jian-Jie Liang ; Anthony Yu ; Alexander Shtukenberg ; Laura N. Poloni ; Vladyslav Kholodovych ; Jay A. Tischfield ; David S. Goldfarb ; Michael D. Ward ; Amrik Sahota
• 刊名：Journal of Medicinal Chemistry
• 出版年：2016
• 出版时间：August 11, 2016
• 年：2016
• 卷：59
• 期：15
• 页码：7293-7298
• 全文大小：469K
• 年卷期：0
• ISSN：1520-4804

文摘

l-Cystine bismorpholide (1a) 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.