Development of autotaxin inhibitors: A series of zinc binding triazoles.

Christopher G Thomson,Darren Le Grand,Mark Dowling,Cara E Brocklehurst, Colin Chinn,Lucy Elphick,Michael Faller,Mark Freeman, Vikki Furminger, Cornelia Gasser, Ahmed Hamadi,Elizabeth Hardaker,Victoria Head,Johan C Hill,Diana I Janus, David Pearce, Anne-Sophie Poulaud,Emily Stanley,Lilya Sviridenko

Bioorganic & Medicinal Chemistry Letters（2018）

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Abstract

•PF-8380 has been used as a template to design a new series of ATX inhibitors.•Reduction of crystallinity was key to improving solubility of the new series.•Selectivity and good oral exposure was achieved with this series.•Compound 12 shows a direct PK-PD relationship with inhibition of production of LPA.

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Key words

Autotaxin inhibition,Idiopathic pulmonary fibrosis,PK/PD,Solubility,hERG inhibition

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