13 research outputs found
Rodent selectivity of piperidine-4-yl-1H-indoles, a series of CC chemokine receptor-3 (CCR3) antagonists: Insights from a receptor model
Rapid synthesis of novel isoindolo[1,2-a]quinazoline on ionic liquid support under microwave irradiation
Small Molecule Receptor Agonists and Antagonists of CCR3 Provide Insight into Mechanisms of Chemokine Receptor Activation
Three-Component Domino Synthesis of 2-Arylquinazoline-4-amines in One Pot by Activating an sp3 C-H Bond in a Nonmetal Catalytic Oxidation System
Unravelling the mechanisms underpinning chemokine receptor activation and blockade by small molecules: a fine line between agonism and antagonism?
Towards small-molecule CXCR3 ligands with clinical potential
The CXCR3 chemokine receptor was first discovered in 1996 and has been shown to play an important role in several diseases, most of which are related to inflammation. This review describes in detail the development of small CXCR3 ligands and their therapeutic potential. Classes of CXCR3 antagonists with strikingly variable core structures have emerged. Some of these compounds have confirmed the beneficial role of CXCR3 antagonism in animal models of disease. One of the compounds, AMG487, progressed to Phase II clinical trials but has been withdrawn because of lack of efficacy. New antagonist classes are being developed to reveal the full therapeutic potential of CXCR3. © 2008 Wiley-VCH Verlag GmbH & Co. KGaA