Studies on Novel Pyridine and 2-pyridone Derivatives of N-arylpiperazine as α-adrenoceptor Ligands

ISSN: 1875-6638 (Online)
ISSN: 1573-4064 (Print)

Volume 13, 8 Issues, 2017

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Medicinal Chemistry

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Studies on Novel Pyridine and 2-pyridone Derivatives of N-arylpiperazine as α-adrenoceptor Ligands

Medicinal Chemistry, 10(2): 144-153.

Author(s): Marzena Baran, Elzbieta Kepczynska, Marek Zylewski, Agata Siwek, Marek Bednarski and Marek Tadeusz Cegla.

Affiliation: Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland.


This paper describes the synthesis of a series of new N-arylpiperazine derivatives of pyridine and 2-pyridone. The in vitro pharmacological study indicated that all of the compounds possess affinity towards α 1-adrenoceptors, with exception of 6d, and are selective over α 2 receptor. The most potent compound 5f displayed 62-fold α 2/ α 1 selectivity with Ki value of 27.3 nM for α 1 receptor. Selectivity of other ligands ranged from 6 to more than 146-fold. Hydrochlorides of selected compounds with the best α 1-adrenoceptor affinity (7b, 7e, 7f, 8b) were tested in vivo (hypotensive activity test in rats) and the results proved their α -adrenoreceptor antagonistic activity. Furthermore, the lipophilicity of the investigated compounds has been assessed experimentally and in silico.


α-adrenoceptor ligands, N-arylpiperazine derivatives, lipophilicity, pyridine, 2-pyridone.

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Article Details

Volume: 10
Issue Number: 2
First Page: 144
Last Page: 153
Page Count: 10
DOI: 10.2174/0929867320999131122114922
Price: $58

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