Dipeptidyl nitrile inhibitors of Cathepsin L

  • Bioorg Med Chem Lett. 2009 Aug 1;19(15):4280-3. doi: 10.1016/j.bmcl.2009.05.071.
Nabil Asaad  1 ,  Paul A Bethel ,  Michelle D Coulson ,  Jack E Dawson ,  Susannah J Ford ,  Stefan Gerhardt ,  Matthew Grist ,  Gordon A Hamlin ,  Michael J James ,  Emma V Jones ,  Galith I Karoutchi ,  Peter W Kenny ,  Andrew D Morley ,  Keith Oldham ,  Neil Rankine ,  David Ryan ,  Stuart L Wells ,  Linda Wood ,  Martin Augustin ,  Stephan Krapp ,  Hannes Simader ,  Stefan Steinbacher
Affiliations
  • 1. Respiratory & Inflammation Research Area, AstraZeneca, Mereside, Alderley Park, Macclesfield SK10 4TG, UK.
PMID: 19515558 DOI: 10.1016/j.bmcl.2009.05.071
Abstract

A series of potent Cathepsin L inhibitors with good selectivity with respect to other cysteine Cathepsins is described and SAR is discussed with reference to the crystal structure of a protein-ligand complex.

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