The Preparation of Macrocyclic Calpain Inhibitors by Ring Closing Metathesis and Cross Metathesis *
AUSTRALIAN JOURNAL OF CHEMISTRY（2014）
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 45nM) 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 2000nM) which reflects an unusually subtle importance of the P2 residue for active site binding.
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Key words
colloids,supramolecular chemistry,macromolecules,ionic liquids,amino acids,polymer chemistry,reaction mechanisms,catalysis,sensors,peptide,analytical chemistry,structure,ab initio calculations,inorganic chemistry,biosensors,educational,proteins,spectroscopy,enzymes,kinetics,organic chemistry,physical chemistry,electrochemistry,quantum chemistry,biological chemistry,nanotechnology,density functional theory,self assembly,combinatorial chemistry,pharmaceutical chemistry,surface chemistry,green chemistry,interfaces,photochemistry,crystal structures,mass spectrometry,medicinal chemistry,crystallography,biocatalysis,computational chemistry,combinatorial
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