Novel 2-imidazoles as potent and selective α1A adrenoceptor partial agonists

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Abstract

Novel 2-imidazoles have been identified as potent partial agonists of the α1A adrenergic receptor, with good selectivity over the α1B, α1D and α2A receptor sub-types. Sulfonamide 23 possessed attractive drug-like properties with respect to physicochemical and ADME properties and wide ligand selectivity.

Graphical abstract

A series of novel 2-imidazoles is described, which combine potent and selective α1A partial agonist pharmacology with good drug-like properties.

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Acknowledgments

We thank Alison Bridgeland for screening data; Debbie Lovering, Edward Pegden, Danny Ho, Katherine England and Helen Mason for compound synthesis. We also thank Peter Bungay for ADME assessment of compound 23.

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