Quinonic derivatives active against a virulent strain of Toxoplasma gondii. Synthesis of 2-methylfuro[2,3-g]- and [3,2-g]isoquinolinetriones

P Nebois; M E Sarciron; B Bibal; B Bouammali; O Cherkaoui; F Pautet; A F Pétavy; N Walchshofer; H Fillion

doi:10.1016/s0960-894x(00)00112-8

Quinonic derivatives active against a virulent strain of Toxoplasma gondii. Synthesis of 2-methylfuro[2,3-g]- and [3,2-g]isoquinolinetriones

Bioorg Med Chem Lett. 2000 May 1;10(9):871-3. doi: 10.1016/s0960-894x(00)00112-8.

Authors

P Nebois¹, M E Sarciron, B Bibal, B Bouammali, O Cherkaoui, F Pautet, A F Pétavy, N Walchshofer, H Fillion

Affiliation

¹ Laboratoire de Chimie Organique EA 635, Université Claude Bernard, Faculté de Pharmacie, Lyon, France.

PMID: 10853649
DOI: 10.1016/s0960-894x(00)00112-8

Abstract

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.

MeSH terms

Animals
Antiprotozoal Agents / chemical synthesis*
Antiprotozoal Agents / pharmacology
Cell Line
Furans / chemical synthesis*
Furans / pharmacology
Humans
Monocytes / drug effects
Monocytes / parasitology
Quinolines / chemical synthesis*
Quinolines / pharmacology
Toxoplasma / drug effects*
Toxoplasma / growth & development

Substances

Antiprotozoal Agents
Furans
Quinolines