1.
Bioorg Med Chem Lett
; 14(9): 2163-7, 2004 May 03.
Article
in English
| MEDLINE
| ID: mdl-15081001
ABSTRACT
The present manuscript details the discovery and early fundamental structure-activity relationship studies involving compound 3, a novel hydroxyethylene peptide isostere derived molecule that provides micromolar inhibition of CCL3 binding to its receptor CCR1. Initial studies established this screening hit as a legitimate lead for further medicinal chemistry optimization.
Subject(s)
Peptides/pharmacology , Receptors, Chemokine/antagonists & inhibitors , Crystallography, X-Ray , Peptides/chemistry , Protein Conformation , Receptors, CCR1
2.
Bioorg Med Chem Lett
; 14(9): 2169-73, 2004 May 03.
Article
in English
| MEDLINE
| ID: mdl-15081002
ABSTRACT
The present manuscript details structure-activity relationship studies of lead structure 1, which led to the discovery of CCR1 antagonists >100-fold more potent than 1.
Subject(s)
Receptors, Chemokine/antagonists & inhibitors , Cell Line , Humans , Receptors, CCR1 , Structure-Activity Relationship
3.
Bioorg Med Chem Lett
; 14(9): 2175-9, 2004 May 03.
Article
in English
| MEDLINE
| ID: mdl-15081003
ABSTRACT
The synthesis, biological activity, and pharmacokinetic profile of novel CCR1 antagonists are described.
