Forty new aminoalkanol derivatives with potential anticonvulsant activity were designed and synthesized. In vivo studies (mice, intraperitoneal administration) showed anticonvulsant activity (maximal electroshock seizure test, MES test) of nineteen compounds, (ED50 values and protective indices PI ranging 22.62–78.30 mg/kg b.w. and 1.78–4.25, respectively). Compounds 30 (R,S‐1‐((2‐(2‐(2‐chloro‐5‐methylphenoxy)ethoxy)ethyl)amino)propan‐2‐ol), 31 (R,S‐2‐((2‐(2‐(2‐chloro‐5‐methylphenoxy)ethoxy)ethyl)amino)propan‐1‐ol) and 33 (S enantiomer of 31) showed relatively low ED50 values (26.45–34.26 mg/kg b.w.) accompanied by PI indexes above 3. Compounds 30 and 31 were investigated in terms of mechanism of action (5‐HT1A receptors binding assay and in silico database screening) and safety against gastrointestinal flora (both compounds proved safe). An integral part of the study was also a comprehensive structure‐activity relationship, including current and previously obtained results for aminoalkanol derivatives.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.