Autor: |
Payne, Richard J., Brown, Karina M., Coxon, James M., Morton, James D., Lee, Hannah Yun-Young, Abell, Andrew D. |
Zdroj: |
Australian Journal of Chemistry; 2004, Vol. 57 Issue: 9 p877-884, 8p |
Abstrakt: |
We present a new synthesis of SJA6017 (a potent m-calpain inhibitor) and its adaptation in order to prepare analogues in which the constituent Leu and Val residues are systematically replaced with their corresponding ?-amino acids and/or the N-terminal fluorophenylsulfonyl group is replaced by a water solubilizing N-pyridin-3-ylmethoxycarbonyl group. All compounds have been assayed against m-calpain, and the best inhibitor, SJA6017, has been shown to inhibit the development of opacity in a lens culture system design to mimic cataract. |
Databáze: |
Supplemental Index |
Externí odkaz: |
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