1.
Bioorg Med Chem Lett
; 22(21): 6694-9, 2012 Nov 01.
Article
in English
| MEDLINE
| ID: mdl-23021991
ABSTRACT
The discovery and optimisation of a series of zwitterionic CCR3 antagonists is described. Optimisation of the structure led to AZ12436092, a compound with excellent selectivity over activity at hERG and outstanding pharmacokinetics in preclinical species.
Subject(s)
Drug Discovery , Piperidines/chemistry , Piperidines/pharmacokinetics , Receptors, CCR3/antagonists & inhibitors , Animals , Humans , Inhibitory Concentration 50 , Molecular Structure , Rats
2.
J Med Chem
; 50(24): 5882-5, 2007 Nov 29.
Article
in English
| MEDLINE
| ID: mdl-17963373
ABSTRACT
A novel series of antagonists of the human P2X7 receptor is described. Modification of substituents enabled identification of compounds selective for the rat P2X7 receptor and provides useful pharmacological tools for evaluation of the role of P2X7 in disease.