Synthesis of new 3-alkoxy-7-amino-4-chloro-isocoumarin derivatives as new β-amyloid peptide production inhibitors and their activities on various classes of protease

…, O Pourquié, F Checler, A Thellend, P Pierre…

Index: Bihel, Frederic; Quelever, Gilles; Lelouard, Hugues; Petit, Agnes; Da Costa, Cristine Alves; Pourquie, Olivier; Checler, Frederic; Thellend, Annie; Pierre, Philippe; Kraus, Jean-Louis Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 14 p. 3141 - 3152

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Citation Number: 48

Abstract

A series of new 7-substituted-4-chloro-3-alkoxy isocoumarin derivatives were synthesized and evaluated as inhibitors of representative classes of proteases: serine protease (α- chymotrypsin, trypsin), cysteine protease (Caspase-3), and aspartyl protease (HIV- protease), 20S proteasome and also as inhibitors of amyloid peptide γ-secretase-mediated production. Protease inhibition selectivity is directly related to the structure of the ...