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|Title:||The preparation of macrocyclic calpain inhibitors by ring closing metathesis and cross metathesis|
|Citation:||Australian Journal of Chemistry, 2014; 67(9):1257-1263|
|Seth A. Jones, Joanna Duncan, Steven G. Aitken, James M. Coxon and Andrew D. Abell|
|Abstract:||Ring closing metathesis and cross metathesis approaches to a new macrocyclic peptidomimetic aldehyde 2 have been developed, with the former route being the most convenient. Aldehyde 2 is a potent inhibitor of calpain II (IC50 of 45 nM) with comparable activity to the benchmark acyclic inhibitor SJA6017 4. Both compounds contain an N-terminal 4-fluorophenylsulfonyl group. The P2 Ile analogue of 2 (16) is significantly less active (IC50 of 2000 nM) which reflects an unusually subtle importance of the P2 residue for active site binding.|
|Rights:||Copyright status unknown|
|Appears in Collections:||IPAS publications|
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