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Optimization of Novel Antagonists to the Neurokinin-3 Receptor for the Treatment of Sex-Hormone Disorders (Part II)

[Image: see text] Further lead optimization on N-acyl-triazolopiperazine antagonists to the neurokinin-3 receptor (NK(3)R) based on the concurrent improvement in bioactivity and ligand lipophilic efficiency (LLE) is reported. Overall, compound 3 (LLE > 6) emerged as the most efficacious in castra...

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Detalles Bibliográficos
Autores principales:	Hoveyda, Hamid R., Fraser, Graeme L., Dutheuil, Guillaume, El Bousmaqui, Mohamed, Korac, Julien, Lenoir, François, Lapin, Alexey, Noël, Sophie
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	American Chemical Society 2015
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4499830/ https://www.ncbi.nlm.nih.gov/pubmed/26191358 http://dx.doi.org/10.1021/acsmedchemlett.5b00117

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