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BIM-46174 fragments as potential ligands of G proteins

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Abstract

The 5,6,7,8-tetrahydroimidazo[1,2-a]pyrazine derivative BIM-46174 has received attention as Gαq inhibitor. We conducted structural reductions to monocyclic and bicyclic substructures to explore the chemical space of BIM fragments and to gain insights into the pharmacophore of BIM-type Gαq inhibitors. Two piperazin-2-one-containing fragments and a small library of bicyclic lactams featuring fused pyrazine and diazepine rings were synthesized and evaluated. The results of a second messenger-based cellular assay indicate that the entire BIM structure is required for efficient Gαq inhibition.

Graphical abstract: BIM-46174 fragments as potential ligands of G proteins

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Publication details

The article was received on 10 May 2019, accepted on 16 Aug 2019 and first published on 21 Aug 2019


Article type: Research Article
DOI: 10.1039/C9MD00269C
Med. Chem. Commun., 2019, Advance Article

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    BIM-46174 fragments as potential ligands of G proteins

    J. Küppers, T. Benkel, S. Annala, G. Schnakenburg, E. Kostenis and M. Gütschow, Med. Chem. Commun., 2019, Advance Article , DOI: 10.1039/C9MD00269C

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