Design, synthesis and in vivo evaluation of sodium 2-benzyl-chloromalonates as new central nervous system depressants

作者: Andreia Aguiar Vieira , Bruno Guimarães Marinho , Luana Gonçalves de Souza , Patricia Dias Fernandes , José D. Figueroa-Villar

DOI: 10.1039/C5MD00187K

关键词:

摘要: This work describes the design, synthesis and in vivo evaluation of new central nervous system depressing agents that show low levels acute toxicity as well high solubility water exhibit anxiolytic hypnotic effects. These compounds are sodium 2-benzyl-2-chloromalonates, which were designed using molecular modelling techniques synthesized four steps, with an overall yield between 41% 65%. In tests mice, including pentobarbital-induced sleep, rotarod, open field elevated plus maze tests, carried out, results indicated some these induce activities similar to those induced by diazepam but lower potency greater potency. also orally administered mice doses 2 g kg−1, their effects evaluated for 14 days. The did not signs intoxication, confirming 2-benzyl-2-chloromalonates toxicity. observations indicate analogues efficient safer drugs relative existing standards care.

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