- N-Arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B
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To improve the pharmacokinetics of a previously reported series of dipeptidyl nitrile cathepsin B inhibitors, the P2-P3 amide group was replaced with an arylamine. Further optimization of this template resulted in highly potent and s
- Greenspan, Paul D.,Clark, Kirk L.,Cowen, Scott D.,McQuire, Leslie W.,Tommasi, Ruben A.,Farley, David L.,Quadros, Elizabeth,Coppa, David E.,Du, Zengming,Fang, Zheng,Zhou, Huanghai,Doughty, John,Toscano, Karen T.,Wigg, Andrew M.,Zhou, Siyuan
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p. 4121 - 4124
(2007/10/03)
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- N-substituted peptidyl nitriles as cysteine cathepsin inhibitors
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Compounds of the formula (I), wherein R1 is aryl or biaryl; R2 is aryl-lower alkyl, biaryl-lower alkyl, benzo-fused cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C2-C7/sub
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