Paper
l-Cystine Diamides as l-Cystine Crystallization Inhibitors for Cystinuria.
Published Jul 26, 2016 · DOI · Longqin Hu, Yanhui Yang, Herve Aloysius
Journal of medicinal chemistry
29
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Abstract
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.
L-cystine bismorpholide (1a) and l-cystine bis(N'-methylpiperazide) (1b) show potential as effective inhibitors of cystinuria crystallization, with potential for clinical use in cystinuria treatment.
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