Dipeptide nitrile inhibitors of cathepsin K
Copyright policy )Dipeptide nitrile inhibitors of cathepsin K
A series of dipeptidyl nitriles as inhibitors of cathepsin K have been explored starting from lead structure 1 (Cbz-Leu-NH-CH2-CN, IC50 = 39 nM). Attachment of non-natural amino acid side chains in P1 and modification of the P3 subunit led to inhibitors with higher potency and improved pharmacokinetic properties.
- Novartis (Switzerland) Switzerland
Molecular Structure, Cathepsin K, Drug Evaluation, Preclinical, Stereoisomerism, Dipeptides, In Vitro Techniques, Cathepsins, Rats, Structure-Activity Relationship, Nitriles, Microsomes, Liver, Animals, Humans, Enzyme Inhibitors
Molecular Structure, Cathepsin K, Drug Evaluation, Preclinical, Stereoisomerism, Dipeptides, In Vitro Techniques, Cathepsins, Rats, Structure-Activity Relationship, Nitriles, Microsomes, Liver, Animals, Humans, Enzyme Inhibitors
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