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

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

Journal Name: Medicinal Chemistry

Volume 10 , Issue 2 , 2014

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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 α1-adrenoceptors, with exception of 6d, and are selective over α2 receptor. The most potent compound 5f displayed 62-fold α2/α1 selectivity with Ki value of 27.3 nM for α1 receptor. Selectivity of other ligands ranged from 6 to more than 146-fold. Hydrochlorides of selected compounds with the best α1-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.

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

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Article Details

Year: 2014
Published on: 21 November, 2013
Page: [144 - 153]
Pages: 10
DOI: 10.2174/0929867320999131122114922
Price: $65

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