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Antimicrobial Agents and Chemotherapy, January 2003, p. 174-180, Vol. 47, No. 1
0066-4804/03/$08.00+0     DOI: 10.1128/AAC.47.1.174-180.2003
Copyright © 2003, American Society for Microbiology. All Rights Reserved.

In Vitro Activities of 7-Substituted 9-Chloro and 9-Amino-2-Methoxyacridines and Their Bis- and Tetra-Acridine Complexes against Leishmania infantum

Carole Di Giorgio,1* Florence Delmas,1 Nathalie Filloux,2 Maxime Robin,2 Laetitia Seferian,2 Nadine Azas,1 Monique Gasquet,1 Muriel Costa,1 Pierre Timon-David,1 and Jean-Pierre Galy2

Laboratoire de Parasitologie, Hygiène et Zoologie, Faculté de Pharmacie, Marseille Cedex 05,1 Laboratoire de Valorisation de la Chimie Fine, Université d'Aix-Marseille III, Site de Saint Jérome, Marseilles, France2

Received 28 May 2002/ Returned for modification 1 August 2002/ Accepted 17 September 2002

9-Chloro and 9-amino-2-methoxyacridines bearing different substituents in position 7, as well as their corresponding unsubstituted dimeric and tetrameric complexes, were investigated for in vitro antiproliferative properties against Leishmania infantum compared to toxicity towards human monocytes. The results clearly confirmed that several compounds of the 2-methoxyacridine series, together with their corresponding dimeric and tetrameric derivatives, had strong in vitro antiparasitic properties. Antileishmanial activity was shown to depend on the nature of both 7- and 9-substituted groups in monoacridines, while it varied according to the nature of the 9-substituted group and the length of the linker among bis- and tetra-acridines. The effects of acridine derivatives on DNA synthesis raised the hypothesis that DNA metabolism constituted their main target in Leishmania promastigotes; however, secondary effects on other biochemical pathways, including protein and lipid metabolism, were observed, suggesting that acridine compounds could be considered multitarget drugs.

* Corresponding author. Mailing address: Laboratoire de Parasitologie, Hygiène et Zoologie, Faculté de Pharmacie, 27 Bd. Jean Moulin, 13385 Marseille Cedex 05, France. Phone: 33.04.91.83.55.44. Fax: 33.04.91.80.26.12. E-mail: Carole.Digiorgio{at}Pharmacie.univ-mrs.fr.

Antimicrobial Agents and Chemotherapy, January 2003, p. 174-180, Vol. 47, No. 1
0066-4804/03/$08.00+0     DOI: 10.1128/AAC.47.1.174-180.2003
Copyright © 2003, American Society for Microbiology. All Rights Reserved.



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