PMID: 11900863Mar 20, 2002Paper

Synthesis, antiarrhythmic, and antihypertensive effects of novel 1-substituted pyrrolidin-2-one and pyrrolidine derivatives with adrenolytic activity

European Journal of Medicinal Chemistry
B MalawskaL Antkiewicz-Michaluk

Abstract

A series of 1-substituted pyrrolidin-2-one and pyrrolidine derivatives were synthesised and tested for electrocardiographic, antiarrhythmic, and antihypertensive activity as well as for alpha(1)- and alpha(2)-adrenoceptors binding affinities. Among the newly synthesised derivatives several compounds with 3-(4-arylpiperazin-1-yl)propyl moiety displayed strong antiarrhythmic (7a-12a) and antihypertensive (7a-11a) activities. Compound 11a, 1-[2-acetoxy-3-[4-(2-methoxyphenyl)piperazin-1-yl]propyl]pyrrolidin-2-one, was the most potent in this series. The pharmacological results and binding studies suggest that their antiarrhythmic and hypotensive effects may be related to their alpha-adrenolytic properties, and that those properties depend on the presence of the 1-phenylpiperazine moiety with a methoxy- or chloro- substituent in the ortho position in the phenyl ring.

Citations

Feb 7, 2012·Medicinal Chemistry Research : an International Journal for Rapid Communications on Design and Mechanisms of Action of Biologically Active Agents·Alicja Nowaczyk, Katarzyna Kulig
Oct 16, 2010·Naunyn-Schmiedeberg's Archives of Pharmacology·Jacek SapaKatarzyna Kulig
Apr 26, 2016·European Journal of Medicinal Chemistry· Shagufta, Irshad Ahmad
Dec 2, 2004·European Journal of Medicinal Chemistry·Tomasz DylagKatarzyna Kieć-Kononowicz
May 21, 2008·Bioorganic & Medicinal Chemistry·Jadwiga HandzlikKatarzyna Kieć-Kononowicz

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