Exploration of peptidyl hydrazones as water-soluble calpain inhibitors
1Research Laboratory, Senju Pharmaceutical Co., Ltd., 1-5-4 Murotani Nishiku, Kobe 651-2241, Japan. masayuki-nakamura@senju.co.jp
Bioorganic & Medicinal Chemistry Letters
|June 1, 2002
Abstract:
A series of peptidyl hydrazones was synthesized, and their inhibitory activity against mu-calpain and water-solubility were measured. Among these compounds, N,N-dimethyl glycyl hydrazone 6, which inhibited mu-calpain with IC(50) of 0.37 microM, possessed the appropriate water-solubility. Furthermore, hydrazone 6 was found to possess the excellent in vitro metabolic stability.


