Influence of the Terminal Amide Fragment Geometry in Some 3-Arylideneindolin-2 (1H)-ones on Their 5-HT 1A/5-HT 2A Receptor Activity

…, S Charakchieva-Minol, A Kozioł, A Kłodzińska…

Index: Mokrosz, Maria J.; Charakchieva-Minol, Sijka; Koziol, Aneta; Klodzinska, Aleksandra; Chojnacka-Wojcik, Ewa Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 9 p. 1229 - 1231

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Citation Number: 8

Abstract

Several 1, 4-disubstituted arylpiperazine derivatives of 3-arylideneindolin-2 (1H)-one (Z and E isomers) were tested for their 5-HT1A and 5-HT2A receptor activity in vitro and in vivo. It was shown that introduction of 3-arylidene substituents to indolin-2 (1H)-one moiety allowed to change the mixed 5-HT1A/5-HT2A receptor ligands to 5-HT2A ones with antagonistic in vivo activity.