Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds

Abstract

In the course of studies on tranquilizers, new non-benzodiazepine-like compounds were synthesized. These are 1-(3,4,5-trimethoxyphenoxy)-3-[4-(2-methoxyphenyl)piperazinyl]prop an-2-ol (INN: enciprazine) and derivatives thereof which were screened pharmacologically in order to evaluate their central nervous system activity. Compounds with marked antiaggressive and anxiolytic properties but without dependence potential could be detected. Enciprazine was selected for clinical investigations.

Novel quinoline and naphthalene derivatives as potent antimycobacterial agents

“…Etherification of alcohol 20 [36] with epi-chlorohydrin using NaH as a base in dry DMF gave oxirane 21 (52%). Nucleophilic opening of the oxirane ring in 21 was carried out by treating compound 21 with appropriate aryl-piperazines [37] in refluxing iso-propanol for 16 h to furnish the target compounds 22-30 ( Fig. 4) in moderate yields (23-44%).…”