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Antimicrobial Agents and Chemotherapy, August 2002, p. 2588-2594, Vol. 46, No. 8
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.8.2588-2594.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.

In Vitro Activities of Position 2 Substitution-Bearing 6-Nitro- and 6-Amino-Benzothiazoles and Their Corresponding Anthranilic Acid Derivatives against Leishmania infantum and Trichomonas vaginalis

Florence Delmas,¹ Carole Di Giorgio,^1* Maxime Robin,² Nadine Azas,¹ Monique Gasquet,¹ Claire Detang,² Muriel Costa,¹ Pierre Timon-David,¹ and Jean-Pierre Galy²

Laboratoire de Parasitologie, Hygiène et Zoologie, Faculté de Pharmacie, Université d'Aix-Marseille II, Marseille Cedex 05,¹ Laboratoire de Valorisation de la Chimie Fine, Université d'Aix-Marseille III, Marseille Cedex 20, France²

Received 13 February 2002/ Returned for modification 10 April 2002/ Accepted 14 May 2002

6-Nitro- and 6-amino-benzothiazoles bearing different chains in position 2 and their corresponding anthranilic acid derivatives were investigated for their in vitro antiparasitic properties against parasites of the species Leishmania infantum and Trichomonas vaginalis compared to their toxicity towards human monocytes. Biological investigations established that the antiprotozoal properties depended greatly on the chemical structure of the position 2 substitution-bearing group. Compound C1, 2-[(2-chloro-benzothiazol-6-yl) amino] benzoic acid, demonstrated an interesting antiproliferative activity towards parasites of the species T. vaginalis, while compound C11, 2-({2-[(2-hydroxyethyl) amino]-benzothiazol-6-yl} amino) benzoic acid, exhibited a promising activity against parasites of the species L. infantum in their intracellular amastigote form. Additional experiments established that compound C11, which was poorly toxic against the promastigote and the extracellular amastigote forms of the parasite, could improve host-protective mechanisms against Leishmania by preventing parasite internalization by macrophages and stimulating NO production, by means of a mechanism synergistically enhanced by the presence of gamma interferon.

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

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Antimicrobial Agents and Chemotherapy, August 2002, p. 2588-2594, Vol. 46, No. 8
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.8.2588-2594.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.

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