The discovery of structurally novel CCR1 antagonists derived from a hydroxyethylene peptide isostere template.
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.
Crystallography, X-Ray↗