Synthesis and biological evaluation of new heterocyclic quinolinones as anti-parasite and anti-HIV drug candidates.
We have synthesized quinolinones with potential antiparasitic and anti-HIV activities by an original two-step method involving microwave irradiation and have evaluated their activities against Plasmodium falciparum, Leishmania donovani, Trichomonas vaginalis, and HIV. None of the tested compounds had been previously described using this method of synthesis. One of the compounds had interesting antiparasitic and anti-HIV activity, which could be improved by substitution with different radicals.
Darque
Albert
A
UMR-MD3-Relations Hôte-Parasites, Pharmacologie et Thérapeutique, Faculté de Pharmacie, Université de la Méditerranée, Marseille Cedex 05, France.
Dumètre
Aurélien
A
Hutter
Sébastien
S
Casano
Gilles
G
Robin
Maxime
M
Pannecouque
Christophe
C
Azas
Nadine
N
D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D000977:Antiparasitic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D006575:Heterocyclic Compounds, 3-Ring / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D006801:Humans; D007893:Leishmania donovani / Q000187:drug effects; D009000:Monocytes / Q000187:drug effects / Q000276:immunology; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D014246:Trichomonas vaginalis / Q000187:drug effects
D019380:Anti-HIV Agents; D000977:Antiparasitic Agents; D006575:Heterocyclic Compounds, 3-Ring; D015363:Quinolones