Discovery of Spirofused Piperazine and Diazepane Amides as Selective Histamine‑3 Antagonists with in Vivo Efficacy in a Mouse Model of Cognition

A new series of potent and selective histamine-3 receptor (H3R) antagonists was identified on the basis of an azaspiro[2.5]octane carboxamide scaffold. Many scaffold modifications were largely tolerated, resulting in nanomolar-potent compounds in the H3R functional assay. Exemplar compound 6s demons...

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