Synthesis and antianxiety activity of (.omega.-piperazinylalkoxy)indan derivatives
摘要:
A series of (omega-piperazinylalkoxy)indan derivatives has been synthesized and screened for potential antianxiety activities. The effect of structural modification of these molecules on activities has been systemically examined. Antianxiety activity was displayed by 5-[3-(4-phenyl-1-piperazinyl)propoxy]indan (2), 5-[3-[4-(4-fluorophenyl)-1-piperazinyl]-propoxy]indan (8), 6-fluoro-5-[3-(4-phenyl-1-piperazinyl)propoxy]indan (33), and 6-methyl-5-[3-(4-phenyl-1-piperazinyl)propoxy]indan (42), as determined in antifighting and anti-morphine tests. These derivatives in antianxiety tests were equipotent or more potent than chlordiazepoxide with less muscle-relaxant effect. They also showed weak neuroleptic-like action.
DOI:
10.1021/jm00356a024
作为产物:
描述:
3-ethyl-5-methoxy-indane 、 吡啶盐酸盐 在
氯仿 作用下,
以
水 为溶剂,
反应 5.0h,
以gave 32 g of 3-ethyl-5-hydroxy-indane的产率得到3-Aethyl-5-hydroxyindan
A series of (omega-piperazinylalkoxy)indan derivatives has been synthesized and screened for potential antianxiety activities. The effect of structural modification of these molecules on activities has been systemically examined. Antianxiety activity was displayed by 5-[3-(4-phenyl-1-piperazinyl)propoxy]indan (2), 5-[3-[4-(4-fluorophenyl)-1-piperazinyl]-propoxy]indan (8), 6-fluoro-5-[3-(4-phenyl-1-piperazinyl)propoxy]indan (33), and 6-methyl-5-[3-(4-phenyl-1-piperazinyl)propoxy]indan (42), as determined in antifighting and anti-morphine tests. These derivatives in antianxiety tests were equipotent or more potent than chlordiazepoxide with less muscle-relaxant effect. They also showed weak neuroleptic-like action.
Indan-5-yl-N-methylcarbamic acid esters
申请人:Bayer Aktiengesellschaft
公开号:US04107324A1
公开(公告)日:1978-08-15
Indan-5-yl-N-methylcarbamic acid esters of the formula ##STR1## in which R represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sup.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sup.2 represents C.sub.1 -C.sub.4 alkyl, R.sup.3 represents hydrogen or C.sub.1 -C.sub.4 alkyl and R.sup.4 represents hydrogen, chlorine, bromine, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, Which possess arthropodicidal and fungicidal properties.