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).
Download
Full text not available from this repository.
Description/Abstract
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.
| Item Type: | Article |
|---|---|
| Related URLs: | |
| Keywords: | combinatorial chemistry, discovery, target |
| Subjects: | Q Science Q Science > QD Chemistry |
| Divisions: | University Structure - Pre August 2011 > School of Chemistry |
| Item ID: | 19944 |
| Date Deposited: | 17 Feb 2006 |
| Last Modified: | 01 Jun 2011 03:57 |
| Contributors: | De Luca, S. (Author) Ulhaq, S. (Author) Dixon, M. J. (Author) Essex, J. (Author) Bradley, M. (Author) |
| Date: | 7 April 2003 |
| Status: | Published |
| URI: | http://eprints.soton.ac.uk/id/eprint/19944 |
Actions (login required)
 |
View Item |
