Synthesis and antiparasitic activity of new 1-nitro, 1-amino and 1-acetamido 9-acridinones.
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.
Ngadi
L
L
Groupe d'Enseignement et de Recherche en Chimie Thérapeutique Organique et Physique U.R.A. C.N.R.S. 1411, Faculté de Pharmacie, Marseille.
Bsiri
N G
NG
Mahamoud
A
A
Galy
A M
AM
Galy
J P
JP
Soyfer
J C
JC
Barbe
J
J
Placidi
M
M
Rodriguez-Santiago
J I
JI
Mesa-Valle
C
C
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
D000166:Acridines; D000609:Aminoacridines; D000981:Antiprotozoal Agents