1. Pharmacological evaluation of a novel series of urea, thiourea and guanidine derivatives as P2X 7 receptor antagonists
- Author
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James O'Brien-Brown, Michael Kassiou, Tristan A. Reekie, Sarah L. Bowyer, Erick C.N. Wong, and Eryn L. Werry
- Subjects
0301 basic medicine ,Stereochemistry ,Aryl ,Organic Chemistry ,Clinical Biochemistry ,Pharmaceutical Science ,Biochemistry ,03 medical and health sciences ,chemistry.chemical_compound ,030104 developmental biology ,0302 clinical medicine ,chemistry ,Thiourea ,Drug Discovery ,Urea ,Molecular Medicine ,Potency ,Moiety ,Guanidine ,Molecular Biology ,P2x7 receptor ,Linker ,030217 neurology & neurosurgery - Abstract
We report on P2X7 receptor antagonists based on a lead adamantly-cyanoguanidine-aryl moiety. We have investigated the importance of the central cyanoguanidine moiety by replacing it with urea, thiourea or guanidine moieties. We have also investigated the linker length between the central moiety and the aryl portion. All compounds were assessed for their inhibitory potency in a pore-formation dye uptake assay at the P2X7 receptor. None of the compounds resulted in an improved potency illustrating the importance of the cyanoguanidine moiety in this chemotype.
- Published
- 2017
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