The role of polycyclic frameworks in modulating P2X7 receptor function |
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| Authors: | Timothy B. Callis,Tristan A. Reekie,James O&#x Brien-Brown,Erick C.N. Wong,Eryn L. Werry,Nabiha Elias,William T. Jorgensen,John Tsanaktsidis,Louis M. Rendina,Michael Kassiou |
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| Affiliation: | 1. School of Chemistry, The University of Sydney, NSW, 2006, Australia;2. School of Medical Sciences, The University of Sydney, NSW, 2006, Australia;3. Faculty of Health Sciences, The University of Sydney, NSW, 2006, Australia;4. CSIRO Manufacturing, Clayton South, Victoria 3169, Australia |
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| Abstract: | Herein we describe our recent attempts to target the P2X7 receptor for potential treatment of neurological disorders. This work focusses on different polycycles including carborane, adamantane or cubane, joined by either a cyanoguanidine or an amide linker to phenyl or isoquinoline moieties. We have demonstrated the superiority of the adamantyl moiety over other polycycles in terms of synthetic accessibility and biological (cellular) activity. We have also shown that an amide or cyanoguanidine linker can greatly alter the biological activity of compounds. This SAR study provides important insights into the types of functionality required to target the P2X7 receptor. |
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| Keywords: | Polycyclic Structure-activity relationships Isoquinoline Cyanoguanidine |
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