Fibroblast growth factor receptor modulators employing diamines with reduced phospholipidosis-inducing potential

[Display omitted] SUN13837 (1), a fibroblast growth factor receptor modulator, has been an attractive candidate for treating neurodegenerative diseases. However, one of its metabolites, N-benzyl-4-(methylamino)piperidine (BMP), turned out to possess phospholipidosis-inducing potential (PLIP) in vitr...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2020-07, Vol.28 (14), p.115562-115562, Article 115562
Hauptverfasser:	Sakai, Hiroki, Inoue, Hidekazu, Murata, Kenji, Toba, Tetsuya, Shimmyo, Yoshiari, Narii, Nobuhiro, Ueno, Shin-ya, Igawa, Yoshiyuki, Takemoto, Naohiro
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Brain Kp Caco-2 Cells Diamines - chemical synthesis Diamines - chemistry Diamines - pharmacology Dose-Response Relationship, Drug FGFR modulator Humans Male Microsomes, Liver - chemistry Microsomes, Liver - metabolism Molecular Structure Neurons - drug effects Neurons - metabolism Neuroprotective Agents - chemical synthesis Neuroprotective Agents - chemistry Neuroprotective Agents - pharmacology P-gp PAMPA Phospholipidosis Phospholipids - antagonists & inhibitors Phospholipids - metabolism Rats Rats, Wistar Receptors, Fibroblast Growth Factor - metabolism Structure-Activity Relationship
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