Identification of Triazolopyridines as Selective α5-GABAA Receptor Negative Allosteric Modulators by a Hybridization Approach.

György Szabó, Benedek Imre Károlyi, Ágnes Gyöngyvér Vaskó, Attila Potor, Krisztina Vukics, Gábor László Kapus, László Fodor, Amrita Bobok, Mónika Vastag, Imre Bata

ACS chemical neuroscience 2023 Jan 04

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The identification and characterization of novel triazolopyridine derivatives with selective α5 subunit-containing GABAA receptor negative allosteric modulator (NAM) activity are disclosed. As a result of in silico screening of our corporate compound deck, we identified a moderately potent hit that was converted to an advanced hit bearing better physicochemical and pharmacological properties using a hybridization approach. Subsequent optimization led to the identification of in vitro potent and subtype-selective α5-GABAA receptor NAMs representing a new chemotype in this area.

Citation

György Szabó, Benedek Imre Károlyi, Ágnes Gyöngyvér Vaskó, Attila Potor, Krisztina Vukics, Gábor László Kapus, László Fodor, Amrita Bobok, Mónika Vastag, Imre Bata. Identification of Triazolopyridines as Selective α5-GABAA Receptor Negative Allosteric Modulators by a Hybridization Approach. ACS chemical neuroscience. 2023 Jan 04;14(1):148-158