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Synthesis and biological evaluation of phosphate Prodrugs of 4-Phospho-D-erythronohydroxamic acid, an inhibitor of 6-phosphogluconate dehydrogenase

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Synthesis and biological evaluation of phosphate Prodrugs of 4-Phospho-D-erythronohydroxamic acid, an inhibitor of 6-phosphogluconate dehydrogenase. / Ruda, Gian Filippo; Alibu, Vincent P.; Mitsos, Christos; Bidet, Olivier; Kaiser, Marcel; Brun, Reto; Barrett, Michael P.; Gilbert, Ian H.

In: ChemMedChem, Vol. 2, No. 8, 08.2007, p. 1169-1180.

Research output: Contribution to journalArticle

Harvard

Ruda, GF, Alibu, VP, Mitsos, C, Bidet, O, Kaiser, M, Brun, R, Barrett, MP & Gilbert, IH 2007, 'Synthesis and biological evaluation of phosphate Prodrugs of 4-Phospho-D-erythronohydroxamic acid, an inhibitor of 6-phosphogluconate dehydrogenase' ChemMedChem, vol 2, no. 8, pp. 1169-1180.

APA

Ruda, G. F., Alibu, V. P., Mitsos, C., Bidet, O., Kaiser, M., Brun, R., Barrett, M. P., & Gilbert, I. H. (2007). Synthesis and biological evaluation of phosphate Prodrugs of 4-Phospho-D-erythronohydroxamic acid, an inhibitor of 6-phosphogluconate dehydrogenase. ChemMedChem, 2(8), 1169-1180doi: 10.1002/cmdc.200700040

Vancouver

Ruda GF, Alibu VP, Mitsos C, Bidet O, Kaiser M, Brun R et al. Synthesis and biological evaluation of phosphate Prodrugs of 4-Phospho-D-erythronohydroxamic acid, an inhibitor of 6-phosphogluconate dehydrogenase. ChemMedChem. 2007 Aug;2(8):1169-1180.

Author

Ruda, Gian Filippo; Alibu, Vincent P.; Mitsos, Christos; Bidet, Olivier; Kaiser, Marcel; Brun, Reto; Barrett, Michael P.; Gilbert, Ian H. / Synthesis and biological evaluation of phosphate Prodrugs of 4-Phospho-D-erythronohydroxamic acid, an inhibitor of 6-phosphogluconate dehydrogenase.

In: ChemMedChem, Vol. 2, No. 8, 08.2007, p. 1169-1180.

Research output: Contribution to journalArticle

Bibtex - Download

@article{fa698bb08cd846d8a4380eb17bb29c3b,
title = "Synthesis and biological evaluation of phosphate Prodrugs of 4-Phospho-D-erythronohydroxamic acid, an inhibitor of 6-phosphogluconate dehydrogenase",
author = "Ruda, {Gian Filippo} and Alibu, {Vincent P.} and Christos Mitsos and Olivier Bidet and Marcel Kaiser and Reto Brun and Barrett, {Michael P.} and Gilbert, {Ian H.}",
year = "2007",
volume = "2",
number = "8",
pages = "1169--1180",
journal = "ChemMedChem",
issn = "1860-7179",

}

RIS (suitable for import to EndNote) - Download

TY - JOUR

T1 - Synthesis and biological evaluation of phosphate Prodrugs of 4-Phospho-D-erythronohydroxamic acid, an inhibitor of 6-phosphogluconate dehydrogenase

A1 - Ruda,Gian Filippo

A1 - Alibu,Vincent P.

A1 - Mitsos,Christos

A1 - Bidet,Olivier

A1 - Kaiser,Marcel

A1 - Brun,Reto

A1 - Barrett,Michael P.

A1 - Gilbert,Ian H.

AU - Ruda,Gian Filippo

AU - Alibu,Vincent P.

AU - Mitsos,Christos

AU - Bidet,Olivier

AU - Kaiser,Marcel

AU - Brun,Reto

AU - Barrett,Michael P.

AU - Gilbert,Ian H.

PY - 2007/8

Y1 - 2007/8

N2 - <p>We have previously reported the discovery of potent and selective inhibitors of 6-phosphogluconate dehydrogenase, the third enzyme of the phosphate pentose pathway, from Trypanosoma brucei, the causative organism of human African trypanosomiasis. These inhibitors were charged phosphate derivatives with restricted capacity to enter cells. Herein, we report the synthesis of five different classes of prodrugs: phosphoramidate; bis-S-acylthioethyl esters (bis-SATE); bis-pivaloxymethyl (bis-POM); CycloSaligenyl; and phenyl, S-acyl thioethyl mixed phosphate esters (mix-SATE). Prodrugs were studied for stability and activity against the intact parasites. Most prodrugs caused inhibition of the growth of the parasites. The activity of the prodrugs against the parasites appeared to be related to their stability in aqueous buffer.</p>

AB - <p>We have previously reported the discovery of potent and selective inhibitors of 6-phosphogluconate dehydrogenase, the third enzyme of the phosphate pentose pathway, from Trypanosoma brucei, the causative organism of human African trypanosomiasis. These inhibitors were charged phosphate derivatives with restricted capacity to enter cells. Herein, we report the synthesis of five different classes of prodrugs: phosphoramidate; bis-S-acylthioethyl esters (bis-SATE); bis-pivaloxymethyl (bis-POM); CycloSaligenyl; and phenyl, S-acyl thioethyl mixed phosphate esters (mix-SATE). Prodrugs were studied for stability and activity against the intact parasites. Most prodrugs caused inhibition of the growth of the parasites. The activity of the prodrugs against the parasites appeared to be related to their stability in aqueous buffer.</p>

UR - http://ukpmc.ac.uk/articles/PMC2248282

U2 - 10.1002/cmdc.200700040

DO - 10.1002/cmdc.200700040

M1 - Article

JO - ChemMedChem

JF - ChemMedChem

SN - 1860-7179

IS - 8

VL - 2

SP - 1169

EP - 1180

ER -

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