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
下载
收藏
页码：336 / 345
页数：10
相关论文
共 50 条
  • [1] The design, synthesis and biological evaluation of novel prodrugs for the treatment of cystinosis
    Kay, G.
    Cairns, D.
    McCaughan, B.
    Warasiha, B.
    JOURNAL OF PHARMACY AND PHARMACOLOGY, 2007, 59 : A7 - A8
  • [2] Synthesis and in vitro evaluation of novel pro-drugs for the treatment of nephropathic cystinosis
    Omran, Ziad
    Moloney, Kevin A.
    Benylles, Amina
    Kay, Graeme
    Knott, Rachel M.
    Cairns, Donald
    BIOORGANIC & MEDICINAL CHEMISTRY, 2011, 19 (11) : 3492 - 3496
  • [3] A potential new prodrug for the treatment of cystinosis: Design, synthesis and in-vitro evaluation
    McCaughan, Bridgeen
    Kay, Graeme
    Knott, Rachel M.
    Cairns, Donald
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (05) : 1716 - 1719
  • [4] Design, synthesis and in vitro evaluation of novel water-soluble prodrugs of buparvaquone
    Mäntylä, A
    Rautio, J
    Nevalainen, T
    Keski-Rahkonen, P
    Vepsälainen, J
    Järvinen, T
    EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2004, 23 (02) : 151 - 158
  • [5] Synthesis and in vitro evaluation of bisphosphonated glycopeptide prodrugs for the treatment of osteomyelitis
    Tanaka, Kelly S. E.
    Dietrich, Evelyne
    Ciblat, Stephane
    Metayer, Claude
    Arhin, Francis F.
    Sarmiento, Ingrid
    Moeck, Gregory
    Parr, Thomas R., Jr.
    Far, Adel Rafai
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 20 (04) : 1355 - 1359
  • [6] Bisphosphonate prodrugs:: Synthesis and in vitro evaluation of novel clodronic acid dianhydrides as bioreversible prodrugs of clodronate
    Ahlmark, M
    Vepsäläinen, J
    Taipale, H
    Niemi, R
    Järvinen, T
    JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (08) : 1473 - 1476
  • [7] Design, synthesis and evaluation of novel cyclophosphamide prodrugs for reductive activation.
    Jiang, YY
    Yu, CZ
    Han, JY
    Browne, P
    Knox, RJ
    Hu, LQ
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2003, 226 : U46 - U46
  • [8] Bisphosphonate prodrugs:: Synthesis and in vitro evaluation of novel acyloxyalkyl esters of clodronic acid
    Niemi, R
    Vepsäläinen, J
    Taipale, H
    Järvinen, T
    JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (24) : 5053 - 5058
  • [9] Synthesis and evaluation of novel prodrugs of naproxen
    Prabodh Chander Sharma
    Sonia Yadav
    Rakesh Pahwa
    Dhirender Kaushik
    Sandeep Jain
    Medicinal Chemistry Research, 2011, 20 : 648 - 655
  • [10] Synthesis and evaluation of novel prodrugs of naproxen
    Sharma, Prabodh Chander
    Yadav, Sonia
    Pahwa, Rakesh
    Kaushik, Dhirender
    Jain, Sandeep
    MEDICINAL CHEMISTRY RESEARCH, 2011, 20 (05) : 648 - 655
12345