Isoxazole-tethered diarylheptanoid analogs: Discovery of a new drug-like PAR2 antagonist.

Debnath Bhuniya,Sandeep Bhosale,Satyanarayana B Reddy, Sudharshan N Reddy

Bioorganic & Medicinal Chemistry Letters（2018）

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摘要

•Design of a new class of isoxazole-tethered diarylheptanoid analogs.•Stereo-conserved access to syn and anti-1,3-diol features starting from d-glucose.•Significantly improved in vitro drug-like properties compared to curcumin-I.•Structurally distinct and phytochemical based PAR2 antagonist scaffold.•Highlighted analog 4a with PAR2 IC50: 6 μM (HEK293 cells, trypsin agonist).

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关键词

Diarylheptanoid,Stereo-conserved synthesis,Isoxazole tether,Protease-activated receptor-2 (PAR2) antagonist

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