Scaffold hopping of fused piperidine-type NK3 receptor antagonists to reduce environmental impact

Add time:07/11/2019    Source:sciencedirect.com

Neurokinin-3 receptor (NK3R) plays a pivotal role in the release of gonadotropin-releasing hormone in the hypothalamus–pituitary–gonadal (HPG) axis. To develop novel NK3R antagonists with less environmental toxicity, a series of heterocyclic scaffolds for the triazolopiperazine substructure in an NK3R antagonist fezolinetant were designed and synthesized. An isoxazolo[3,4–c]piperidine derivative exhibited moderate NK3R antagonistic activity and favorable properties that were decomposable under environmental conditions.

We also recommend Trading Suppliers and Manufacturers of 2-(3,4-DIMETHOXYBENZYL)PIPERIDINE (cas 102458-70-8). Pls Click Website Link as below: cas 102458-70-8 suppliers

Prev:Discovery of indolin-2-one derivatives as potent PAK4 inhibitors: Structure-activity relationship analysis, biological evaluation and molecular docking study
Next:Organic light-emitting diodes based on 9-(2-naphthyl)anthracene derivatives with a triphenylsilane unit as the deep-blue emitting layer)