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Bioorg Med Chem Lett ; 30(16): 127325, 2020 08 15.
Artículo en Inglés | MEDLINE | ID: mdl-32631530

RESUMEN

As part of the presented research, thirteen new aminoalkanol derivatives were designed and obtained by chemical synthesis. In vivo studies (mice, i.p.) showed anticonvulsant activity (MES) of nine compounds, and in the case of one compound (R,S-trans-2-((2-(2,3,5-trimethylphenoxy)ethyl)amino)cyclohexan-1-ol, 4) both anticonvulsant (ED50 MES = 15.67 mg/kg, TD50 rotarod = 78.30 mg.kg, PI = 5.00) and analgesic activity (OXA-induced neuropathic pain, active at 15 mg/kg). For selected active compounds additional in vitro studies have been performed, including receptor studies (5-HT1A), evaluation of antioxidant activity (DPPH assay), metabolism studies as well as safety panel (mutagenicity, safety in relation to the gastrointestinal flora, cytotoxicity towards astrocytes as well as impact on their proliferation and cell cycle).


Asunto(s)
Amino Alcoholes/farmacología , Analgésicos/farmacología , Anticonvulsivantes/farmacología , Antioxidantes/farmacología , Neuralgia/tratamiento farmacológico , Amino Alcoholes/química , Analgésicos/química , Analgésicos/metabolismo , Animales , Anticonvulsivantes/química , Anticonvulsivantes/metabolismo , Antioxidantes/química , Antioxidantes/metabolismo , Compuestos de Bifenilo/antagonistas & inhibidores , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Humanos , Estructura Molecular , Picratos/antagonistas & inhibidores , Relación Estructura-Actividad
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