title: Synthesis and antiparasitic activity of new 1-nitro, 1-amino and 1-acetamido 9-acridinones.
abstract: 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.
authors.affiliation: Groupe d'Enseignement et de Recherche en Chimie Thérapeutique Organique et Physique U.R.A. C.N.R.S. 1411, Faculté de Pharmacie, Marseille.
authors.forename: L
authors.initials: L
authors.lastname: Ngadi
authors.forename: N G
authors.initials: NG
authors.lastname: Bsiri
authors.forename: A
authors.initials: A
authors.lastname: Mahamoud
authors.forename: A M
authors.initials: AM
authors.lastname: Galy
authors.forename: J P
authors.initials: JP
authors.lastname: Galy
authors.forename: J C
authors.initials: JC
authors.lastname: Soyfer
authors.forename: J
authors.initials: J
authors.lastname: Barbe
authors.forename: M
authors.initials: M
authors.lastname: Placidi
authors.forename: J I
authors.initials: JI
authors.lastname: Rodriguez-Santiago
authors.forename: C
authors.initials: C
authors.lastname: Mesa-Valle
mesh_terms: D000048:Acanthamoeba / Q000187:drug effects; D000166:Acridines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000609:Aminoacridines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D015496:CD4-Positive T-Lymphocytes / Q000187:drug effects; D007893:Leishmania donovani / Q000187:drug effects; D008297:Male; D051379:Mice; D014349:Trypanosoma cruzi / Q000187:drug effects
chemical_list: D000166:Acridines; D000609:Aminoacridines; D000981:Antiprotozoal Agents