The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine.

Peter Lin,Lehua Chang,Robert J Devita,Jonathan R Young,Ronsar Eid,Xinchun Tong,Song Zheng,Richard G Ball,Nancy N Tsou,Gary G Chicchi,Marc M Kurtz,Kwei-Lan C Tsao,Alan Wheeldon,Emma J Carlson,Waisi Eng,H Donald Burns,Richard J Hargreaves,Sander G Mills

Bioorganic & Medicinal Chemistry Letters（2007）

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摘要

SAR studies on amides, ureas, and vinylogous amides derived from pyrrolidine led to the discovery of several potent hNK1 antagonists. One vinylogous amide (45b) had excellent potency, selectivity, pharmacokinetic profile, and functional activity in vivo. An in vivo rhesus macaque brain receptor occupancy PET study for compound 45b revealed an estimated Occ90∼300ng/ml.

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关键词

NK1,Neurokinin NK1 antagonist,Tachykinin NK1 antagonist,Substance P antagonist

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