Synthesis of 2-substituted trifluoromethylquinolines for the evaluation of leishmanicidal activity

被引:44
作者
Dade, J
Provot, O
Moskowitz, H
Mayrargue, J
Prina, E
机构
[1] Univ Paris Sud, UPRES A CNRS 8076, Fac Pharm, Chim Organ Lab, F-92296 Chatenay Malabry, France
[2] Inst Pasteur, Unite Immunophysiol & Parasitisme Intracellulaire, F-75724 Paris 15, France
关键词
leishmaniasis; 2-propyltrifluoromethylquinoline; 2-epoxypropyltrifluoromethylquinoline; 2-(propen-1-yl)-trifluoromethylquinoline;
D O I
10.1248/cpb.49.480
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of 2-substituted-trifluoromethylquinolines from aniline, trifluoromethylanilines, 3-amino-quinoline and trifluoromethylquinaldines is reported. In vitro antileishmanial evaluation of 2-alkyl, 2-alkenyl and 2-epoxypropyl-trifluoromethylquinolines is presented.
引用
收藏
页码:480 / 483
页数:4
相关论文
共 12 条
[1]   HOMOLOGATION OF FURFURAL AND DERIVATIVES TO FURYLACETALDEHYDES [J].
BROCHET, C ;
SYSSA, JL ;
MOULOUNGUI, Z ;
DELMAS, M ;
GASET, A .
SYNTHETIC COMMUNICATIONS, 1991, 21 (17) :1735-1741
[2]   RECENT DEVELOPMENTS IN THE CHEMOTHERAPY OF LEISHMANIASIS [J].
CROFT, SL .
TRENDS IN PHARMACOLOGICAL SCIENCES, 1988, 9 (10) :376-381
[3]   CHIMANINES, NEW 2-SUBSTITUTED QUINOLINES, ISOLATED FROM AN ANTIPARASITIC PLANT IN BOLIVIA - GALIPEA-LONGIFLORA [J].
FOURNET, A ;
HOCQUEMILLER, R ;
ROBLOT, F ;
CAVE, A ;
RICHOMME, P ;
BRUNETON, J .
JOURNAL OF NATURAL PRODUCTS, 1993, 56 (09) :1547-1552
[4]   Determination of 2-n-propylquinoline in mouse plasma and liver by high-performance liquid chromatography [J].
Iglarz, M ;
Baune, B ;
Gantier, JC ;
Hocquemiller, R ;
Farinotti, R .
JOURNAL OF CHROMATOGRAPHY B, 1998, 714 (02) :335-340
[5]  
KOBAYASHI Y, 1970, CHEM PHARM BULL, V18, P2334
[6]   A CONVENIENT TRIFLUOROMETHYLATION OF AROMATIC HALIDES WITH SODIUM TRIFLUOROACETATE [J].
MATSUI, K ;
TOBITA, E ;
ANDO, M ;
KONDO, K .
CHEMISTRY LETTERS, 1981, (12) :1719-1720
[7]   Regioselectivity of Rhodococcus NCIMB 11216 epoxide hydrolase: Applicability of E-values for description of enantioselectivity depends on substrate structure [J].
Mischitz, M ;
Mirtl, C ;
Saf, R ;
Faber, K .
TETRAHEDRON-ASYMMETRY, 1996, 7 (07) :2041-2046
[8]  
MUNOS MH, 1994, CHEM PHARM BULL, V42, P1914, DOI 10.1248/cpb.42.1914
[9]  
MUNOS MH, 1997, THESIS U PARIS SUD
[10]   IMPROVED SYNTHESIS OF QUINALDINES BY THE SKRAUP REACTION [J].
SONG, ZG ;
MERTZMAN, M ;
HUGHES, DL .
JOURNAL OF HETEROCYCLIC CHEMISTRY, 1993, 30 (01) :17-21