Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists

[Display omitted] The optimization efforts that led to a novel series of methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones that are potent rat and human P2X7 antagonists are described. These efforts resulted in the discovery of compounds with good drug-like properti...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2015-08, Vol.25 (16), p.3157-3163
Hauptverfasser:	Rudolph, Dale A., Alcazar, Jesus, Ameriks, Michael K., Anton, Ana Belen, Ao, Hong, Bonaventure, Pascal, Carruthers, Nicholas I., Chrovian, Christa C., De Angelis, Meri, Lord, Brian, Rech, Jason C., Wang, Qi, Bhattacharya, Anindya, Andres, Jose Ignacio, Letavic, Michael A.
Format:	Artikel
Sprache:	eng
Schlagworte:	5,6-Dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones Animals CNS Depression Half-Life Humans Microsomes - metabolism P2X7 Protein Binding Purinergic P2X Receptor Antagonists - chemistry Purinergic P2X Receptor Antagonists - metabolism Purinergic P2X Receptor Antagonists - pharmacokinetics Pyrazines - chemistry Rats Receptors, Purinergic P2X7 - chemistry Receptors, Purinergic P2X7 - metabolism Structure-Activity Relationship Triazoles - chemistry
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