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Derivatives of 3‐ sec ‐Butyl‐1‐oxo‐2,3‐dihydroisoquinoline as Inhibitors of μ‐Calpain
Author(s) -
Chicharro Roberto,
Alonso Mercedes,
Mazo M. Teresa,
Arán Vicente J.,
Herradón Bernardo
Publication year - 2006
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200600046
Subject(s) - calpain , chemistry , protease , ic50 , stereochemistry , protease inhibitor (pharmacology) , enzyme , in vitro , biochemistry , biology , immunology , human immunodeficiency virus (hiv) , antiretroviral therapy , viral load
A protein destroyer is blocked : ( S,S,Z )‐methyl‐2‐(3‐ sec ‐butyl‐1‐oxo‐2,3‐dihydroisoquinolin‐4(1 H )‐ylidene)acetate is a potent low‐molecular‐weight inhibitor of μ ‐ calpain (IC 50 =25 n M ). Several derivatives of this compound were synthesized and tested as inhibitors of the calpain protease to gain insight into their structure–activity relationships.