TY - JOUR
T1 - L -Cystine Diamides as l -Cystine Crystallization Inhibitors for Cystinuria
AU - Hu, Longqin
AU - Yang, Yanhui
AU - Aloysius, Herve
AU - Albanyan, Haifa
AU - Yang, Min
AU - Liang, Jian Jie
AU - Yu, Anthony
AU - Shtukenberg, Alexander
AU - Poloni, Laura N.
AU - Kholodovych, Vladyslav
AU - Tischfield, Jay A.
AU - Goldfarb, David S.
AU - Ward, Michael D.
AU - Sahota, Amrik
PY - 2016/8/11
Y1 - 2016/8/11
N2 - 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.
AB - 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.
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U2 - 10.1021/acs.jmedchem.6b00647
DO - 10.1021/acs.jmedchem.6b00647
M3 - Article
C2 - 27409142
AN - SCOPUS:84982156361
VL - 59
SP - 7293
EP - 7298
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 15
ER -