1-[(Imidazolidin-2-yl)imino]-1H-indoles as new hypotensive agents: synthesis and in vitro and in vivo biological studies
Anita Kornicka, Aleksandra Wasilewska, Jarosław Sączewski, Alan L. Hudson, Konrad Boblewski, Artur Lehmann, Karol Gzella, Mariusz Belka, Franciszek Sączewski, Maria Gdaniec, Apolonia Rybczyńska and Tomasz Bączek
Version of Record online: 26 SEP 2016 | DOI: 10.1111/cbdd.12846
1-[(Imidazolidin-2-yl)imino]-1H-indole analogues of a hypotensive α2-AR/imidazoline I1 binding site-selective ligand, 7-fluoro-1-[(imidazolidin-2-yl)imino]-1H-indazole (7-F-marsanidine), were synthesized and tested in vitro for α1- and α2-adrenergic and imidazoline I1 and I2 receptors’ binding affinities as well as in vivo for cardiovascular effects. 7-F-indole 3g, the most potent hypotensive agent in this series, is characterized by higher affinity and selectivity for α2-ARs over I1-IBS than that of 7-F-marsanidine. The newly prepared compounds are found to possess a high metabolic stability in vitro.