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Synthesis and antiplasmodial activity of new 4-aryl-2-trichloromethylquinazolines
Pierre Verhaeghe ,
Nadine Azas ,
Monique Gasquet ,
Sébastien Hutter ,
Christophe Ducros ,
Michèle Laget ,
Sylvain Rault ,
Pascal Rathelot ,
Patrice Vanelle
January 2008
January 2008
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Abstract
A series of original 4-aryl-substituted 2-trichloromethylquinazoline derivatives was
synthesized using a microwave-assisted Suzuki-Miyaura cross-coupling approach. Antiplasmodial
activity was evaluated on both chloroquino-resistant and -sensitive Plasmodium falciparum
strains, and the selectivity indexes for THP1 and HepG2 human cells were also calculated,
revealing their antiplasmodial potential.