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Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists
Authors:Whitlock Gavin A  Conlon Kelly  McMurray Gordon  Roberts Lee R  Stobie Alan  Thurlow Richard J
Affiliation:aDepartment of Chemistry, Pfizer Global Research and Development, Sandwich Labs, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK;bDepartment of Genitourinary Biology, Pfizer Global Research and Development, Sandwich Labs, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK
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.
Keywords:α  1A Adrenoceptor   Partial agonist   Selectivity   2-Imidazole   Drug-like properties
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