Antiparasitic activity of highly conjugated pyrimidine-2,4-dione derivatives

Nadine Azas; Pascal Rathelot; Serge Djekou; Florence Delmas; A Gellis; Carole Di Giorgio; Patrice Vanelle; Pierre Timon-David

doi:10.1016/j.farmac.2003.07.009

Antiparasitic activity of highly conjugated pyrimidine-2,4-dione derivatives

Farmaco. 2003 Dec;58(12):1263-70. doi: 10.1016/j.farmac.2003.07.009.

Authors

Nadine Azas¹, Pascal Rathelot, Serge Djekou, Florence Delmas, A Gellis, Carole Di Giorgio, Patrice Vanelle, Pierre Timon-David

Affiliation

¹ Laboratoire de Parasitologie, EA 864, Faculté de Pharmacie, 27 Boulevard Jean Moulin, 13385 Marseille Cedex 5, France. nadine.azas@pharmacie.univ-mrs.fr

PMID: 14630237
DOI: 10.1016/j.farmac.2003.07.009

Abstract

4-[2-(1,3-Dimethyl-5-nitro-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)vinyl]benzaldehyde was synthesized in four steps from 6-methyl-1H,3H-pyrimidine-2,4-dione. This aldehyde was functionalized by various substituted anilines or substituted benzylamines. Antiparasitic activities of the corresponding azomethines were assessed against Plasmodium falciparum, Trichomonas vaginalis and Leishmania infantum compared to their toxicity versus human cells.

Publication types

Comparative Study
Research Support, Non-U.S. Gov't

MeSH terms

Animals
Antiparasitic Agents / chemistry*
Antiparasitic Agents / pharmacology*
Cell Line, Tumor
Erythrocytes / drug effects
Erythrocytes / parasitology
Humans
Leishmania infantum / drug effects
Leishmania infantum / growth & development
Monocytes / drug effects
Plasmodium falciparum / drug effects
Plasmodium falciparum / growth & development
Pyrimidines / chemistry*
Pyrimidines / pharmacology*
Trichomonas vaginalis / drug effects
Trichomonas vaginalis / growth & development

Substances

Antiparasitic Agents
Pyrimidines