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Solid-phase synthesis of a focused library of trypanothione reductase inhibitors

De Luca, S., Ulhaq, S., Dixon, M. J., Essex, J. and Bradley, M. (2003) Solid-phase synthesis of a focused library of trypanothione reductase inhibitors Tetrahedron Letters, 44, (15), pp. 3195-3197. (doi:10.1016/S0040-4039(03)00438-6).

Record type: Article


A focused library of inhibitors of the enzyme trypanothione reductase was prepared using solid-phase synthesis. The inhibitors were based on a previously identified, non-competitive, lead compound comprising of two Pmc (2,2,5,7,8-pentamethylchroman-6-sulfonyl) side-chain protected, N-capped arginine residues linked by a spermidine bridge. In total six protecting groups and four capping groups were used to generate a 24-membered library. All compounds bearing the 5-methoxyindole-3-acetic acid capping group were found to have good activity. The most potent inhibitor was observed to contain the Mtr (4-methoxy-2,3,6-trimethylbenzenesulphonyl) protecting group on the arginine residue, terminated with tryptophan as the capping group.

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Published date: 7 April 2003
Keywords: combinatorial chemistry, discovery, target


Local EPrints ID: 19944
ISSN: 0040-4039
PURE UUID: 9fac10f3-2aa3-4971-9dc6-fc8229e99082
ORCID for J. Essex: ORCID iD

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Date deposited: 17 Feb 2006
Last modified: 17 Jul 2017 16:30

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Author: S. De Luca
Author: S. Ulhaq
Author: M. J. Dixon
Author: J. Essex ORCID iD
Author: M. Bradley

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