We report the design and synthesis of a new class of piperazine- pyridazinone analogues. The arylpiperazine moiety, the length of the spacer, and the terminal molecular fragment were varied to evaluate their influence in determining the affinity of the new compounds toward the α1- adrenergic receptor (α1-AR), α2-adrenergic receptor (α2-AR), and the 5-HT1A serotoninergic receptor (5-HT1AR). Biological data showed that most of the compounds have an α1-AR affinity in the nanomolar or subnanomolar range, while affinity toward the other two receptors was lower in most cases. However, several of the tested compounds also showed very good (in the nanomolar range) or moderate affinity toward the 5-HT1AR subtype.

Betti, L., Zanelli, M., Giannaccini, G., Manetti, F., Schenone, S., & Strappaghetti, G. (2006). Synthesis of New Piperazine-pyridazinone Derivatives and their Binding Affinity toward alpha1-, alpha2-Adrenergic and 5-HT-1A Serotoninergic Receptors. BIOORGANIC & MEDICINAL CHEMISTRY, 14(8), 2828-2836 [10.1016/j.bmc.2005.12.009].

Synthesis of New Piperazine-pyridazinone Derivatives and their Binding Affinity toward alpha1-, alpha2-Adrenergic and 5-HT-1A Serotoninergic Receptors

MANETTI, FABRIZIO;
2006

Abstract

We report the design and synthesis of a new class of piperazine- pyridazinone analogues. The arylpiperazine moiety, the length of the spacer, and the terminal molecular fragment were varied to evaluate their influence in determining the affinity of the new compounds toward the α1- adrenergic receptor (α1-AR), α2-adrenergic receptor (α2-AR), and the 5-HT1A serotoninergic receptor (5-HT1AR). Biological data showed that most of the compounds have an α1-AR affinity in the nanomolar or subnanomolar range, while affinity toward the other two receptors was lower in most cases. However, several of the tested compounds also showed very good (in the nanomolar range) or moderate affinity toward the 5-HT1AR subtype.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11365/22450
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