1384485-34-0Relevant articles and documents
Synthesis and biological evaluation of optically active Ki16425
Sato, Takanao,Sugimoto, Kenji,Inoue, Asuka,Okudaira, Shinichi,Aoki, Junken,Tokuyama, Hidetoshi
, p. 4323 - 4326 (2012/09/22)
An enantionselective synthesis of both enantiomers of Ki16425, which possesses selective LPA antagonistic activity, was achieved. The isoxazole core was constructed by a 1,3-dipolar cycloaddition of nitrile oxide with alkyne and condensation with the optically active α-phenethyl alcohol segment, which was prepared by an enantioselective reduction of arylmethylketone. Biological evaluation of both enantiomers of Ki16425 revealed that the (R)-isomer showed much higher antagonistic activity for LPA1 and LPA3 receptors.