| 19013793 |
Ueno H, Kawai M, Shimokawa H, Hirota M, Ohmi M, Sudo R, Ohta A, Arano Y, Hattori K, Ohmi T, Kato N, Kojima M, Ueno Y, Yamamoto M, Moriguchi Y, Eda H, Masubuchi K: Synthesis and structure-activity relationships of oxamyl dipeptide caspase inhibitors developed for the treatment of liver disease. Bioorg Med Chem Lett. 2009 Jan 1;19(1):199-202. Epub 2008 Nov 5.
The P4 region of a series of oxamyl dipeptide caspase inhibitors was optimized by the combination of anti-apoptotic activity in the Jurkat/Fas (JFas) cellular assay and membrane permeability in the PAMPA assay. Two highly potent anti-apoptotic agents with moderate membrane permeability, 29 and 36, showed strong in vivo efficacy in a murine model of alpha-Fas-induced liver injury. |
62(0,2,2,2) |