Synthesis and antiparasitic activity of new 1-nitro, 1-amino and 1-acetamido 9-acridinones.

Arzneimittelforschung

Groupe d'Enseignement et de Recherche en Chimie Thérapeutique Organique et Physique U.R.A. C.N.R.S. 1411, Faculté de Pharmacie, Marseille.

Published: April 1993

The synthesis of 1-amino-10-alkyl-9-acridinones 4 and 5 and of homologous 9-thio-acridinones 7 and 8 are described. Similarly, the synthesis of 1-nitro-4-(2'-aminoethylamino)-9-acridinones 13 and 15, is described. Compound 4 was used as starting material for the preparation of 10-alkyl-9-acridinone dimers 6, bridged with an alpha,omega-diamido chain. Compound 15 was selected for biological investigations on pathogenic parasite strains, and a promising antiamoebic activity could be shown.

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