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), 3195-3197. (doi:10.1016/S0040-4039(03)00438-6).
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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.
|Keywords:||combinatorial chemistry, discovery, target|
Q Science > QD Chemistry
|Divisions:||University Structure - Pre August 2011 > School of Chemistry
|Date Deposited:||17 Feb 2006|
|Last Modified:||01 Jun 2011 03:57|
|RDF:||RDF+N-Triples, RDF+N3, RDF+XML, Browse.|
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