Synthesis and Pharmacological Evaluation of New 1??[3??(4??Arylpiperazin??1??yl)??2??hydroxypropyl]??pyrrolidin??2??one Derivatives with Anti??arrhythmic, Hypotensive, and …

…, J Sapa, D Maciag, B Filipek, B Malawska

Index: Kulig, Katarzyna; Sapa, Jacek; Maciag, Dorota; Filipek, Barbara; Malawska, Barbara Archiv der Pharmazie, 2007 , vol. 340, # 9 p. 466 - 475

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Citation Number: 25

Abstract

Abstract A series of novel arylpiperazines bearing a pyrrolidin-2-one fragment was synthesized and evaluated for the binding affinity of the α 1-and α 2-adrenoceptors (AR) and for the antiarrhythmic and hypotensive activities of the compounds. The most potent and selective compound 1-[2-hydroxy-3-[4-[(2-hydroxyphenyl) piperazin-1-yl] propyl] pyrrolidin-2- one 8 binds with pK i= 6.71 for α 1-AR. Derivative 8 was also the most active in the ...