1,3-Diphenylpyrazoles: synthesis and antiparasitic activities of azomethine derivatives

被引:200
作者
Rathelot, P
Azas, N
El-Kashef, H
Delmas, F
Di Giorgio, C
Timon-David, P
Maldonado, J
Vanelle, P
机构
[1] Fac Pharm Marseille, Chim Organ Lab, CNRS, UMR 6517, F-13385 Marseille 5, France
[2] Fac Pharm Marseille, EA 864, Parasitol Lab, F-13385 Marseille, France
[3] Assiut Univ, Fac Sci, Dept Chem, Assiut 71516, Egypt
关键词
diphenylpyrazole; nitrophenylpyrazole; azomethine; antiplasmodial activity; trichmonocidal activity; leishmanicidal activity;
D O I
10.1016/S0223-5234(02)01388-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
1,3-Diphenylpyrazole-4-carboxaldehyde and 1-(4-nitrophenyl)-3-phenylpyrazole-4-carboxaldehyde were obtained from the appropriated phenylhydrazones via the Vilsmeier-Haack reaction. These two aldehydes were functionalized by various substituted anilines or substituted benzylamines. Antiparasitic activities of the corresponding azomethines were assessed. In the most cases, nitrated compounds were found to be more efficient than non-nitrated ones against Plasmodium falciparum, Trichomonas vaginalis and Leishmania infantum. (C) 2002 Published by Editions scientifiques et medicales Elsevier SAS.
引用
收藏
页码:671 / 679
页数:9
相关论文
共 25 条
[21]  
TRAGER W, 1976, SCIENCE, V193, P673, DOI 10.1126/science.781840
[22]   USE OF HYDROETHIDINE AND FLOW-CYTOMETRY TO ASSESS THE EFFECTS OF LEUKOCYTES ON THE MALARIAL PARASITE PLASMODIUM-FALCIPARUM [J].
VANDERHEYDE, HC ;
ELLOSO, MM ;
VANDEWAA, J ;
SCHELL, K ;
WEIDANZ, WP .
CLINICAL AND DIAGNOSTIC LABORATORY IMMUNOLOGY, 1995, 2 (04) :417-425
[23]  
VOGEL AI, 1967, PRACTICAL ORGANIC CH, P743
[24]   Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists [J].
Wustrow, DJ ;
Capiris, T ;
Rubin, R ;
Knobelsdorf, JA ;
Akunne, H ;
Davis, MD ;
MacKenzie, R ;
Pugsley, TA ;
Zoski, KT ;
Heffner, TG ;
Wise, LD .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (16) :2067-2070
[25]   A FLOW CYTOMETRIC METHOD FOR ASSESSING VIABILITY OF INTRAERYTHROCYTIC HEMOPARASITES [J].
WYATT, CR ;
GOFF, W ;
DAVIS, WC .
JOURNAL OF IMMUNOLOGICAL METHODS, 1991, 140 (01) :23-30