In continuing our search for selective α1-adrenoceptor (AR) antagonists, we have synthesized new alkoxyarylpiperazinylalkylpyridazinone derivatives. The new compounds were tested for their affinity toward α1- and α2-AR and toward the 5-HT1A receptor. α1-AR affinity data are in the subnanomolar range, with 3 showing an affinity of 0.052 nM, about 5-fold higher than prazosin. None of the studied compounds was found to be α1/α2 selective, but 8 showed an interesting 5-HT1A/α1 affinity ratio of 119.
L., B., Botta, M., Corelli, F., M., F., G., G., L., M., et al. (2003). Alpha1-Adrenoceptor Antagonists. 6. Structural Optimization of Pyridazinone-Arylpiperazines. Study of the Influence on Affinity and Selectivity of Cyclic Substituents at the Pyridazinone Ring and Alkoxy Groups at the Arylpiperazine Moiety. JOURNAL OF MEDICINAL CHEMISTRY, 46(16), 3555-3558 [10.1021/jm0307842].
Alpha1-Adrenoceptor Antagonists. 6. Structural Optimization of Pyridazinone-Arylpiperazines. Study of the Influence on Affinity and Selectivity of Cyclic Substituents at the Pyridazinone Ring and Alkoxy Groups at the Arylpiperazine Moiety
BOTTA, MAURIZIO;CORELLI, FEDERICO;MANETTI, FABRIZIO;
2003-01-01
Abstract
In continuing our search for selective α1-adrenoceptor (AR) antagonists, we have synthesized new alkoxyarylpiperazinylalkylpyridazinone derivatives. The new compounds were tested for their affinity toward α1- and α2-AR and toward the 5-HT1A receptor. α1-AR affinity data are in the subnanomolar range, with 3 showing an affinity of 0.052 nM, about 5-fold higher than prazosin. None of the studied compounds was found to be α1/α2 selective, but 8 showed an interesting 5-HT1A/α1 affinity ratio of 119.File | Dimensione | Formato | |
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https://hdl.handle.net/11365/22510
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