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XB-ART-41026
Bioorg Med Chem Lett 2009 Oct 01;1919:5746-52. doi: 10.1016/j.bmcl.2009.07.153.
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Discovery of the imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepine scaffold as a novel, potent and selective GABA(A) alpha5 inverse agonist series.

Achermann G , Ballard TM , Blasco F , Broutin PE , Büttelmann B , Fischer H , Graf M , Hernandez MC , Hilty P , Knoflach F , Koblet A , Knust H , Kurt A , Martin JR , Masciadri R , Porter RH , Stadler H , Thomas AW , Trube G , Wichmann J .


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Through iterative design cycles we have discovered a number of novel new classes where the imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepine was deemed the most promising GABA(A) alpha5 inverse agonist class with potential for cognitive enhancement. This class combines a modest subtype binding selectivity with inverse agonism and has the most favourable molecular properties for further lead optimisation towards a central nervous system (CNS) acting medicine.

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