1428308-09-1Relevant articles and documents
TRICYCLIC COMPOUNDS AS KAT II INHIBITORS
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, (2014/01/08)
Compounds of Formula (I), wherein R1, R 2, X1, Y1, Z1, and Z2 are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.
Discovery of hydroxamate bioisosteres as KAT II inhibitors with improved oral bioavailability and pharmacokinetics
Henderson, Jaclyn L.,Sawant-Basak, Aarti,Tuttle, Jamison B.,Dounay, Amy B.,McAllister, Laura A.,Pandit, Jayvardhan,Rong, Suobao,Hou, Xinjun,Bechle, Bruce M.,Kim, Ji-Young,Parikh, Vinod,Ghosh, Somraj,Evrard, Edelweiss,Zawadzke, Laura E.,Salafia, Michelle A.,Rago, Brian,Obach, Ronald S.,Clark, Alan,Fonseca, Kari R.,Chang, Cheng,Verhoest, Patrick R.
, p. 125 - 129 (2013/03/13)
A series of kynurenine aminotransferase II (KAT II) inhibitors has been developed replacing the hydroxamate motif with a bioisostere. Triazolinones or triazoles have proven to be effective replacements with significantly improved pharmacokinetics includin