Synthesis and biological activity of a series of potent fluoromethyl ketone inhibitors of recombinant human calpain I

S Chatterjee, MA Ator, D Bozyczko-Coyne…

Index: Chatterjee, Sankar; Ator, Mark A.; Bozyczko-Coyne, Donna; Josef, Kurt; Wells, Gregory; Tripathy, Rabindranath; Iqbal, Mohamed; Bihovsky, Ron; Senadhi, Shobha E.; Mallya, Satish; O'Kane, Teresa M.; McKenna, Beth Ann; Siman, Robert; Mallamo, John P. Journal of Medicinal Chemistry, 1997 , vol. 40, # 23 p. 3820 - 3828

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Citation Number: 49

Abstract

Calpain I, an intracellular cysteine protease, has been implicated in the neurodegeneration following an episode of stroke. In this paper, we report on a series of potent dipeptide fluoromethyl ketone inhibitors of recombinant human calpain I (rh calpain I). SAR studies revealed that while calpain I tolerates a variety of hydrophobic groups at the P1 site, Leu at P2 is preferred. However, the nature of the N-terminal capping group has a significant ...