Quinonic derivatives active against a virulent strain of Toxoplasma gondii. Synthesis of 2-methylfuro[2,3-g]- and [3,2-g]isoquinolinetriones.
2-methylfuro[2,3-g]isoquinoline-4,7,9-trione (4) and 2-methylfuro[3,2-g]isoquinoline-4,6,9-trione (5) were prepared regiospecifically from 2-azadiene 9 and bromobenzofuran-4,7-diones 1 or 11. The activity of these two compounds and some other quinonic derivatives was evaluated in vitro against a virulent strain of Toxoplasma gondii. Compounds 4 and 7 were found to be as active as pyrimethamine.
Nebois
P
P
Laboratoire de Chimie Organique EA 635, Université Claude Bernard, Faculté de Pharmacie, Lyon, France.
Sarciron
M E
ME
Bibal
B
B
Bouammali
B
B
Cherkaoui
O
O
Pautet
F
F
Pétavy
A F
AF
Walchshofer
N
N
Fillion
H
H
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002460:Cell Line; D005663:Furans / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D009000:Monocytes / Q000187:drug effects / Q000469:parasitology; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D014122:Toxoplasma / Q000187:drug effects* / Q000254:growth & development
D000981:Antiprotozoal Agents; D005663:Furans; D011804:Quinolines