Rational design of novel pyrrolidine derivatives as orally active neurokinin-3 receptor antagonists

The rational design of a novel series of pyrrolidine derivatives as neurokinin-3 receptor antagonists is reported starting from a selective neurokinin-1 receptor antagonist. Typical representatives in this series showed in vivo efficacy after oral administration in a NK3 mediated functional assay. This series of NK3 antagonists shows promise to deliver a novel antipsychotic.

Graphical abstractThe rational design of a novel series of orally active NK3R antagonists is decribed.Figure optionsDownload full-size imageDownload as PowerPoint slide