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1-Aryl-1,2,3,4-tetrahydroisoquinolines as potential antimalarials : synthesis, in vitro antiplasmodial activity and in silico pharmacokinetics evaluation

Hanna, J. N. and Ntie-Kang, F. and Kaiser, M. and Brun, R. and Efange, S. M. N.. (2014) 1-Aryl-1,2,3,4-tetrahydroisoquinolines as potential antimalarials : synthesis, in vitro antiplasmodial activity and in silico pharmacokinetics evaluation. RSC advances, Vol. 4, H. 44 ,22856-22865.

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Official URL: http://edoc.unibas.ch/dok/A6348370

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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
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Kaiser, Marcel and Brun, Reto
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:Royal Society of Chemistry
ISSN:2046-2069
Note:Publication type according to Uni Basel Research Database: Journal article
Last Modified:10 Apr 2015 09:12
Deposited On:10 Apr 2015 09:12

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