3245-55-4Relevant academic research and scientific papers
Synthesis and evaluation of antidepressant-like activity of some 4-substituted 1-(2-methoxyphenyl) piperazine derivatives
Waszkielewicz, Anna M.,Pytka, Karolina,Rapacz, Anna,We?na, Elzbieta,Jarzyna, Monika,Sata?a, Grzegorz,Bojarski, Andrzej,Sapa, Jacek,Zmudzki, Pawe?,Filipek, Barbara,Marona, Henryk
, p. 326 - 335 (2015/03/04)
A series of new derivatives of N-(2-methoxyphenyl) piperazine have been synthesized for their affinity toward serotonergic receptors and for their potential antidepressant-like activity. They have been evaluated toward receptors 5-HT1A, 5-HT6, and 5-HT7, as well as in vivo in the tail suspension, locomotor activity, and motor co-ordination tests. All the tested compounds proved very good affinities toward 5-HT1A and 5-HT7 receptors. The most promising compound was 1-[(2-chloro-6-methylphenoxy)ethoxyethyl]-4-(2-methoxyphenyl) piperazine hydrochloride, exhibiting affinity toward receptors Ki 1A) and Ki = 34 nM (5-HT7). Antidepressant-like activity (tail suspension test) was observed at 2.5 mg/kg b.w. (mice, i.p.), and the effect was stronger than that observed for imipramine (5 mg/kg b.w.). Sedative activity was observed at ED50 (locomotor test, mice, i.p.) = 17.5 mg/kg b.w. and neurotoxicity was observed at TD50 (rotarod, mice, i.p.) = 53.2 mg/kg b.w.
Synthesis and evaluation of anticonvulsant activity of N -(2,5-dimethylphenoxy)-and N-[(2,3,5-trimethylphenoxy)alkyl] aminoalkanols
Waszkielewicz, Anna Maria,Gunia-Krzyzak, Agnieszka,Ceg? A, Marek,Marona, Henryk
, p. 89 - 99 (2015/02/05)
AseriesofnewN-(2,5-dimethylphenoxy)-andN-(2,3,5-trimethylphenoxy)alkylaminoalkanols [I-XVII]wassynthesizedandevaluatedforanticonvulsantactivity.Pharmacologicaltestsincludedmaximal electroshock(MES)andsubcutaneouspentetrazoleseizurethreshold(scMet)assaysaswellasneurotoxicity (TOX)evaluationinmiceafterintraperitoneal(i.p.)administrationand/orinratsafteroral(p.o.)administration. ThemostactivecompoundwasR-2N-[(2,3,5-trimethylphenoxy)ethyl]aminobutan-1-ol,whichexhibited 100%activityinMESatthedoseof30mg/kgbodyweight(mice,i.p.)and75%activityinMESat30mg/kg b.w.(rats,p.o.)withoutneurotoxicityattheactive doses.
Selectivity in alkylation of phenols with 1-bromo-3-chloropropane using phase-transfer catalysis
Reinholz,Becker,Hagenbruch,Schafer,Schmitt
, p. 1069 - 1071 (2007/10/02)
The use of various phase-transfer catalysts in the alkylation of phenol and substituted phenols with 1-bromo-3-chloropropane was investigated. When a quarternary ammonium salt of the general formula R'4N+ X-, where R' = alkyl with a minimum chain length of 4 was used, a mixture of 1-aryloxy-3-chloropropane and 1-aryloxy-3-bromopropane resulted. The effect of counterion, added potassium bromide, and catalysts other than quarternary ammonium salts were assessed for the halopropylation of 2,5-dimethylphenol.
