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

✍ Scribed by Stefania De Luca; Saraj Ulhaq; Mark J. Dixon; Jonathan Essex; Mark Bradley

Book ID
104253302
Publisher
Elsevier Science
Year
2003
Tongue
French
Weight
164 KB
Volume
44
Category
Article
ISSN
0040-4039

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✦ Synopsis

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-3acetic 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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