Identification of novel 1,2,3,6-tetrahydropyridyl-substituted benzo[d]thiazoles: Lead generation and optimization toward potent and orally active EP1 receptor antagonists

[Display omitted] Herein we described the design, synthesis and evaluation of a novel series of benzo[d]thiazole derivatives toward an orally active EP1 antagonist. Lead generation studies provided benzo[d]thiazole core from the four designed scaffolds. Optimization of this scaffold in terms of EP1...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2017-07, Vol.25 (13), p.3406-3430
Hauptverfasser:	Umei, Kentaro, Nishigaya, Yosuke, Tatani, Kazuya, Kohno, Yasushi, Tanaka, Nobuyuki, Seto, Shigeki
Format:	Artikel
Sprache:	eng
Schlagworte:	Benzo[d]thiazole EP1 antagonist Ligand-lipophilicity efficiency
Online-Zugang:	Volltext
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