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Bioorg Med Chem Lett. 2009 Jun 1;19(11):3118-21. doi: 10.1016/j.bmcl.2009.03.162. Epub 2009 Apr 7.

Potent and selective alpha1A adrenoceptor partial agonists--novel imidazole frameworks.

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  • 1Pfizer Global Research and Development, Sandwich Labs, Sandwich, Kent, UK. gavin.whitlock@pfizer.com


Novel imidazole frameworks have been identified as potent partial agonists of the alpha(1A) adrenergic receptor, with good selectivity over the alpha(1B), alpha(1D) and alpha(2A) receptor sub-types. Nitrile 28 possessed attractive CNS drug-like properties with good membrane permeability and no P-pg mediated efflux. 28 also possessed excellent solubility, metabolic stability and wide ligand selectivity.

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