Spiro-1-benzofuranpiperidinylalkanoic acids as a novel and selective sphingosine S1P5 receptor agonist chemotype.

Axel R Stoit,Jos H M Lange,Hein K A C Coolen, Annemieke Rensink,Adri van den Hoogenband,Arnold P den Hartog, Sjoerd van Schaik,Chris G Kruse

Bioorganic & Medicinal Chemistry Letters（2018）

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摘要

The potent and orally available S1P5 receptor agonist 32 showed high S1P5 receptor selectivities against the S1P1-3 receptor subtypes.

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关键词

S1P5 receptor agonists,Subtype selectivity,Spirocyclic scaffold,Molecular modelling,Homology model,Oral bioavailability,Turbidimetric aqueous solubility,Microsomal stability,Membrane permeation

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