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

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.

SUBMITTER: Hu L

PROVIDER: S-EPMC5774851 | biostudies-literature | 2016 Aug

REPOSITORIES: biostudies-literature

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

Hu Longqin L Yang Yanhui Y Aloysius Herve H Albanyan Haifa H Yang Min M Liang Jian-Jie JJ Yu Anthony A Shtukenberg Alexander A Poloni Laura N LN Kholodovych Vladyslav V Tischfield Jay A JA Goldfarb David S DS Ward Michael D MD Sahota Amrik A

Journal of medicinal chemistry 20160726 15

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 knoc ...[more]

PMID: 27409142

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