A rational design approach has been applied to synthesize a novel class of compounds with affinity for α1 adrenergic receptors (AR). Molecular structures are characterized by a benzimidazolylpyridazinone or an imidazolylpyridazinone moiety, an original fragment in the field of the arylpiperazine compounds with α1-AR blocking properties. A 1.1 nM affinity toward α1-AR was found for compound 3, the most active of this series.
Betti, L., Botta, M., Corelli, F., Floridi, M., Fossa, P., Giannaccini, G., et al. (2002). alpha1-Adrenoceptor Antagonists. Rational Design, Synthesis and Biological Evaluation of New Trazodone-like Compounds. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 12(3), 437-440 [10.1016/S0960-894X(01)00772-7].
alpha1-Adrenoceptor Antagonists. Rational Design, Synthesis and Biological Evaluation of New Trazodone-like Compounds
Botta, Maurizio;Corelli, Federico;Manetti, Fabrizio;
2002-01-01
Abstract
A rational design approach has been applied to synthesize a novel class of compounds with affinity for α1 adrenergic receptors (AR). Molecular structures are characterized by a benzimidazolylpyridazinone or an imidazolylpyridazinone moiety, an original fragment in the field of the arylpiperazine compounds with α1-AR blocking properties. A 1.1 nM affinity toward α1-AR was found for compound 3, the most active of this series.
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https://hdl.handle.net/11365/10468
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