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 Mercachem Galapagos Autotaxin1 72dpi

Our discovery chemistry teams continue to have vital impact on our client's drug development programs.

In collaboration with Galapagos, Mercachem scientists developed synthetic routes to new Autotaxin (ATX) inhibitors. Autotaxin (ATX) is a secreted enzyme playing a major role in the production of lysophosphatidic acid (LPA). The ATX–LPA signaling axis arouses a high interest in the drug discovery industry as it has been implicated in several diseases including cancer, fibrotic diseases, and inflammation.

Jörg Heiermann, Group Leader at Mercachem, explains: "We developed an efficient route to an imidazo[1,2-a]pyridine series of compounds by a Gröbke-Blackburn-Bienaymé multicomponent reaction. The synthesized scaffold had various handles for further subtitution, thus allowing rapid SAR exploration."

Compounds displaying high activity in biochemical and plasma assays were identified. In vivo experiments in rats revealed decreased LPA plasma levels for some analogues.

The complete article can be downloaded here.

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