Design, synthesis and initial in vitro evaluation of novel prodrugs for the treatment of cystinosis

被引：6
|
作者：
Anderson, RJ [1 ]
Cairns, D
Cardwell, WA
Case, M
Groundwater, PW
Hall, AG
Hogarth, L
Jones, AL
Meth-Cohn, O
Suryadevara, P
Tindall, A
Thoene, JG
机构：
[1] Univ Sunderland, Sunderland Pharm Sch, Sunderland SR1 3SD, Durham, England
[2] Univ Newcastle Upon Tyne, No Inst Canc Res, Newcastle Upon Tyne NE2 4AD, Tyne & Wear, England
[3] Tulane Univ, Sch Med, Hayward Genet Ctr, New Orleans, LA 70112 USA
来源：
LETTERS IN DRUG DESIGN & DISCOVERY | 2006年 / 3卷 / 05期
关键词：
cystinosis; prodrugs; GGT; cysteamine; cystamine;
D O I：
10.2174/157018006777574258
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Simple amino acid prodrugs of cysteamine and cystamine were synthesized to overcome the problems of palatability and gastrointestinal irritation, while gamma-glutamyl prodrugs were synthesized to target the parent drug to gamma-glutamyl transpepticlase (GGT). Preliminary cystine-depleting evaluation in vitro suggests further investigation is warranted. Low toxicity of the prodrugs was observed.
引用
收藏
页码：336 / 345
页数：10
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