2-Cyano-pyrimidines: a new chemotype for inhibitors of the cysteine protease cathepsin K

  • J Med Chem. 2007 Feb 22;50(4):591-4. doi: 10.1021/jm0613525.
Eva Altmann  1 ,  Reiner Aichholz ,  Claudia Betschart ,  Thomas Buhl ,  Jonathan Green ,  Osamu Irie ,  Naoki Teno ,  René Lattmann ,  Marina Tintelnot-Blomley ,  Martin Missbach
Affiliations
  • 1. Novartis Institutes of BioMedical Research, CH-4002 Basel, Switzerland.
PMID: 17256925 DOI: 10.1021/jm0613525
Abstract

Starting from the purine lead structure 1, a new series of Cathepsin K inhibitors based on a pyrimidine scaffold have been explored. Investigations of P3 and P2 substituents based on molecular modeling suggestions resulted in potent Cathepsin K inhibitors with an improved selectivity profile over other cathepsins.

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