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https://hdl.handle.net/2440/34884
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Type: | Journal article |
Title: | Peptidic aldehydes based on α- and β-amino acids: synthesis, inhibition of m-calpain, and anti-cataract properties |
Other Titles: | Peptidic aldehydes based on alpha- and beta-amino acids: synthesis, inhibition of m-calpain, and anti-cataract properties |
Author: | Payne, R. Brown, K. Coxon, J. Morton, J. Lee, H. Abell, A. |
Citation: | Australian Journal of Chemistry: an international journal for chemical science, 2004; 57(9):877-884 |
Publisher: | C S I R O Publishing |
Issue Date: | 2004 |
ISSN: | 0004-9425 1445-0038 |
Statement of Responsibility: | Richard J. Payne, Karina M. Brown, James M. Coxon, James D. Morton, Hannah Yun-Young Lee and Andrew D. Abell |
Abstract: | 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 β-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. |
Rights: | © CSIRO 2004 |
DOI: | 10.1071/CH04080 |
Published version: | http://dx.doi.org/10.1071/ch04080 |
Appears in Collections: | Aurora harvest 6 Chemistry publications |
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