Structure−Activity Relationship Study and Drug Profile ofN-(4-Fluorophenylsulfonyl)-l-valyl-l-leucinal (SJA6017) as a Potent Calpain Inhibitor
Journal of Medicinal Chemistry2003Vol. 46(5), pp. 868–871
Citations Over TimeTop 13% of 2003 papers
Jun Inoue, Masayuki Nakamura, Ying-She Cui, Yusuke Sakai, Osamu Sakai, Jeanette R. Hill, Kevin Wang, Po‐wai Yuen
Abstract
Novel N-arylsulfonyldipeptidyl aldehyde derivatives were prepared by DMSO oxidation from the corresponding dipeptide alcohol, and their potencies as calpain inhibitors were evaluated in vitro. Among them, N-(4-fluorophenylsulfonyl)-l-valyl-l-leucinal (8, SJA6017) potently inhibited calpains. 8 also inhibited cathepsin B and L but did not inhibit other cysteine proteases (interleukin 1beta-converting enzyme), serine proteases (trypsin, chymotrypsin, thrombin, factor VIIa, factor Xa), or proteasome. Preliminary cytotoxicity studies of 8 exhibited a relatively safe profile.
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