Design, Synthesis and Initial In Vitro Evaluation of Novel Prodrugs for the Treatment of Cystinosis

R. J. Anderson; D. Cairns; W. A. Cardwell; M. Case; P. W. Groundwater; A. G. Hall; L. Hogarth; A. L. Jones; O. Meth-Cohn; P. Suryadevara

doi:10.2174/157018006777574258

ISSN: 1570-1808
E-ISSN: 1875-628X

Design, Synthesis and Initial In Vitro Evaluation of Novel Prodrugs for the Treatment of Cystinosis
Authors: R. J. Anderson¹, D. Cairns², W. A. Cardwell³, M. Case⁴, P. W. Groundwater⁵, A. G. Hall⁶, L. Hogarth⁷, A. L. Jones⁸, O. Meth-Cohn⁹ and P. Suryadevara¹⁰
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¹ Sunderland Pharmacy School, University of Sunderland, Sunderland, SR1 3SD, UK. ² Sunderland Pharmacy School, University of Sunderland, Sunderland, SR1 3SD, UK. ³ Sunderland Pharmacy School, University of Sunderland, Sunderland, SR1 3SD, UK. ⁴ Sunderland Pharmacy School, University of Sunderland, Sunderland, SR1 3SD, UK. ⁵ Sunderland Pharmacy School, University of Sunderland, Sunderland, SR1 3SD, UK. ⁶ Sunderland Pharmacy School, University of Sunderland, Sunderland, SR1 3SD, UK. ⁷ Sunderland Pharmacy School, University of Sunderland, Sunderland, SR1 3SD, UK. ⁸ Sunderland Pharmacy School, University of Sunderland, Sunderland, SR1 3SD, UK. ⁹ Sunderland Pharmacy School, University of Sunderland, Sunderland, SR1 3SD, UK. ¹⁰ Sunderland Pharmacy School, University of Sunderland, Sunderland, SR1 3SD, UK.
Source: Letters in Drug Design & Discovery, Volume 3, Issue 5, Jul 2006, p. 336 - 345
DOI: https://doi.org/10.2174/157018006777574258
- Available online: 01 Jul 2006

Abstract

Simple amino acid prodrugs of cysteamine and cystamine were synthesized to overcome the problems of palatability and gastrointestinal irritation, while γ-glutamyl prodrugs were synthesized to target the parent drug to γ-glutamyl transpeptidase (GGT). Preliminary cystine-depleting evaluation in vitro suggests further investigation is warranted. Low toxicity of the prodrugs was observed.

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2006-07-01

2025-11-01

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Article Type: Research Article

Keyword(s): cystamine; cysteamine; Cystinosis; GGT; prodrugs

Design, Synthesis and Initial In Vitro Evaluation of Novel Prodrugs for the Treatment of Cystinosis

Abstract

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