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

页码：336 / 345

页数：10

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