Synthesis, SAR study, and biological evaluation of novel 2,3-dihydro-1H-imidazo[1,2-a]benzimidazole derivatives as phosphodiesterase 10A inhibitors

[Display omitted] Phosphodiesterase 10A (PDE10A) inhibitors were designed and synthesized based on the dihydro-imidazobenzimidazole scaffold. Compound 5a showed moderate inhibitory activity and good permeability, but unfavorable high P-glycoprotein (P-gp) liability for brain penetration. We performe...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2019-08, Vol.27 (16), p.3692-3706
Hauptverfasser:	Chino, Ayaka, Honda, Shugo, Morita, Masataka, Yonezawa, Koichi, Hamaguchi, Wataru, Amano, Yasushi, Moriguchi, Hiroyuki, Yamazaki, Mayako, Aota, Masaki, Tomishima, Masaki, Masuda, Naoyuki
Format:	Artikel
Sprache:	eng
Schlagworte:	Brain penetration P-gp liability PDE10A inhibitor Schizophrenia Y-maze
Online-Zugang:	Volltext
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