1.
Bioorg Med Chem Lett
; 19(15): 4280-3, 2009 Aug 01.
Article
in English
| MEDLINE
| ID: mdl-19515558
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.
Subject(s)
Cathepsin L/antagonists & inhibitors , Cathepsin L/chemistry , Nitriles/chemical synthesis , Animals , Cartilage, Articular/pathology , Catalysis , Chemistry, Pharmaceutical/methods , Crystallography, X-Ray/methods , Drug Design , Humans , Ligands , Mice , Mice, Transgenic , Nitriles/chemistry , Nitriles/pharmacology , Peptides/chemical synthesis , Peptides/pharmacology , Proteins/chemistry , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 15(1): 25-8, 2005 Jan 03.
Article
in English
| MEDLINE
| ID: mdl-15582404
ABSTRACT
Investigation of weak screening hits led to the identification of N-alkyl-N-[1-(3,3-diphenylpropyl)piperidin-4-yl]-2-phenylacetamides and N-alkyl-N-[1-(3,3-diphenylpropyl)piperidin-4-yl]-N'-benzylureas as potent, selective ligands for the human CCR5 chemokine receptor.
