Synthesis and antiplasmodial activity of new 4-aryl-2-trichloromethylquinazolines.
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.
Verhaeghe
Pierre
P
Laboratoire de Chimie Organique Pharmaceutique, UMR CNRS 6517, Faculté de Pharmacie, Université de la Méditerranée, 27 Bd. Jean Moulin, 13385 Marseille Cedex 05, France.
Azas
Nadine
N
Gasquet
Monique
M
Hutter
Sébastien
S
Ducros
Christophe
C
Laget
Michèle
M
Rault
Sylvain
S
Rathelot
Pascal
P
Vanelle
Patrice
P
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D002460:Cell Line; D002738:Chloroquine / Q000494:pharmacology; D004351:Drug Resistance; D006801:Humans; D006843:Hydrocarbons, Chlorinated / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D010963:Plasmodium falciparum / Q000187:drug effects; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity
D000962:Antimalarials; D006843:Hydrocarbons, Chlorinated; D011799:Quinazolines; D002738:Chloroquine