Cubyl amides: novel P2X7 receptor antagonists.
Polycyclic amides 2 and 5-9 were successfully synthesised and their lipophilicity profiles were evaluated using reverse-phase HPLC. All synthesised compounds possessed P2X7R antagonistic properties when tested on rat spinal cord microglia cells. Extensive screening for binding to other neuroreceptor subtypes demonstrated their P2X7 selectivity.
School of Chemistry, University of Sydney, NSW 2006, Australia.
Hendra
H
Gunosewoyo
Jun Liu
JL
Guo
Maxwell R
MR
Bennett
Mark J
MJ
Coster
Michael
M
Kassiou
D000577:Amides / Q000737:chemistry*; D000818:Animals; D001549:Benzamides / Q000737:chemistry; D001665:Binding Sites; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002851:Chromatography, High Pressure Liquid; D015195:Drug Design; D006801:Humans; D051379:Mice; D017628:Microglia / Q000378:metabolism; D008956:Models, Chemical; D008968:Molecular Conformation; D058919:Purinergic P2 Receptor Antagonists; D051381:Rats; D018048:Receptors, Purinergic P2 / Q000737:chemistry / Q000502:physiology*; D058486:Receptors, Purinergic P2X7; D013116:Spinal Cord / Q000473:pathology
D000577:Amides; D001549:Benzamides; C546468:P2RX7 protein, human; C546469:P2rx7 protein, mouse; C546470:P2rx7 protein, rat; D058919:Purinergic P2 Receptor Antagonists; D018048:Receptors, Purinergic P2; D058486:Receptors, Purinergic P2X7