Discovery Of Ono-8590580: A Novel, Potent And Selective Gaba(A) Alpha(5) Negative Allosteric Modulator For The Treatment Of Cognitive Disorders

A Lewis, A Beresford,M S Chambers, G Clark, D C Hartley, K L Hirst, M Higashino, S Kawahadara, M Nakanishi,T Saito, A Imagawa,H Habashita, S Maidment,A M Macleod,A P Owens, A Rae, C Rouse, G Wishart

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（2020）

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摘要

The identification and SAR development of a series of negative allosteric modulators of the GABAA alpha 5 receptor is described. This novel series of compounds was optimised to provide analogues with high GABAA alpha 5 binding affinity, high alpha 5 negative allosteric modulatory activity, good functional subtype selectivity and low microsomal turnover, culminating in identification of ONO-8590580.

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关键词

GABAA alpha 5, Negative allosteric modulator, Cognition enhancement, ONO-8590580

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