56961-30-9Relevant articles and documents
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Minajew
, (1926)
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ADAMANTANYL-SUBSTITUTED BENZAMIDE COMPOUNDS AND THEIR USE AS P2X7 RECEPTOR ANTAGONISTS
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Page/Page column 20; 25, (2020/03/15)
The present invention relates to adamantanyl-substituted benzamide compounds and their use as antagonists of the P2X7 purinoreceptor. The invention further relates to methods for the treatment of disease and conditions associated with the P2X7 purinoreceptor.
The role of polycyclic frameworks in modulating P2X7 receptor function
Callis, Timothy B.,Reekie, Tristan A.,O'Brien-Brown, James,Wong, Erick C.N.,Werry, Eryn L.,Elias, Nabiha,Jorgensen, William T.,Tsanaktsidis, John,Rendina, Louis M.,Kassiou, Michael
, p. 1207 - 1219 (2017/11/24)
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.