A rational design approach has been applied to synthesize a novel class of compounds with affinity for a1 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 a1-AR blocking properties. A 1.1 nM affinity toward a1-AR was found for compound 3, the most active of this series.
a1-Adrenoceptor Antagonists. Rational Design, Synthesis and Biological Evaluation of New Trazodone-like Compounds
FOSSA, PAOLA;
2002-01-01
Abstract
A rational design approach has been applied to synthesize a novel class of compounds with affinity for a1 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 a1-AR blocking properties. A 1.1 nM affinity toward a1-AR was found for compound 3, the most active of this series.
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