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Bioorg Med Chem Lett. 2003 Nov 17;13(22):4121-4.

N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B.

Author information

1
Novartis Institute of Biomedical Research, One Health Plaza, East Hanover, NJ 07936, USA. paul.greenspan@mpi.com

Abstract

To improve the pharmacokinetics of a previously reported series of dipeptidyl nitrile cathepsin B inhibitors, the P(2)-P(3) amide group was replaced with an arylamine. Further optimization of this template resulted in highly potent and selective inhibitors with excellent oral availability.

PMID:
14592520
DOI:
10.1016/j.bmcl.2003.08.006
[Indexed for MEDLINE]

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