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1-Aryl-1,2,3,4-tetrahydroisoquinolines as potential antimalarials : synthesis, in vitro antiplasmodial activity and in silico pharmacokinetics evaluation
JournalArticle (Originalarbeit in einer wissenschaftlichen Zeitschrift)
 
ID 2846505
Author(s) Hanna, JN; Ntie-Kang, F; Kaiser, M; Brun, R; Efange, SMN
Author(s) at UniBasel Kaiser, Marcel
Brun, Reto
Year 2014
Title 1-Aryl-1,2,3,4-tetrahydroisoquinolines as potential antimalarials : synthesis, in vitro antiplasmodial activity and in silico pharmacokinetics evaluation
Journal RSC advances
Volume 4
Number 44
Pages / Article-Number 22856-22865
Abstract

In the present study, twenty-one 1-aryl-6-hydroxy-1,2,3,4-tetrahydroisoquinoline (THIQ) analogues were synthesized by base-catalyzed Pictet-Spengler reaction, and tested in vitro against P. falciparum using the [H-3] hypoxanthine incorporation assay. Two compounds were found to be inactive while seventeen compounds displayed moderate antiplasmodial activity and two compounds were found to be highly active (IC50 < 0.2 mu g ml(-1)). The two highly active compounds, 1-(4-chlorophenyl)-6-hydroxyl-1,2,3,4tetrahydroisoquinoline and 6-hydroxyspiro[1,2,3,4-tetrahydroisoquinoline-1:1'-cyclohexane], also displayed low cytotoxicity, against rat skeletal myoblast cells, with CC50 values of 257.6 and 174.2 mu M respectively. These results justify further investigation of simple 1-aryl-1,2,3,4-tetrahydroisoquinolines as potential anti-malarial agents

Publisher Royal Society of Chemistry
ISSN/ISBN 2046-2069
edoc-URL http://edoc.unibas.ch/dok/A6348370
Full Text on edoc No
Digital Object Identifier DOI 10.1039/c3ra46791k
 
   

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