The discovery of novel 3-aryl-indazole derivatives as peripherally restricted pan-Trk inhibitors for the treatment of pain

[Display omitted] •New 3-aryl-indazole derivatives as pan-Trk inhibitors were designed and synthesized.•Substrates for efflux transporter were explored by the Caco-2 assay.•Membrane permeability was increased by lowing basicity.•17c demonstrated restricted brain penetration and good in vivo efficacy...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2019-08, Vol.29 (16), p.2320-2326
Hauptverfasser:	Shirahashi, Hiromitsu, Toriihara, Eisuke, Suenaga, Yoshihito, Yoshida, Hideyuki, Akaogi, Kensuke, Endou, Yukiko, Wakabayashi, Makoto, Takashima, Misato
Format:	Artikel
Sprache:	eng
Schlagworte:	3-Aryl-indazole derivative Efflux transporter pan-Trk inhibitor Peripherally restricted pKa-MB
Online-Zugang:	Volltext
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