Synthesis and antifungal activity of cholesterol-hydrazone derivatives

被引:278
作者
Loncle, C
Brunel, JM
Vidal, N
Dherbomez, M
Letourneux, Y
机构
[1] Univ Paul Cezanne, Fac Sci & Tech St Jerome, Lab Synth & Etude Subst Nat Activ Biol, IMRN,INRA 1111, F-13397 Marseille 20, France
[2] IUT La Rochelle, F-17026 La Rochelle, France
关键词
hydrazone; cholesterol derivatives; antifungal activity; antimicrobial activity;
D O I
10.1016/j.ejmech.2004.07.005
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of hydrazones synthesized from various cholesterol derivatives were evaluated for their in vitro antimicrobial properties against human pathogens. The activity was highly dependent on the structure of the different compounds involved. The best results have been obtained with tosylhydrazone cholesterol derivatives 8 and 9 exhibiting activities against Candida albicans (CIP 1663-80) at a concentration of 1.5 mug/ml. (C) 2004 Elsevier SAS. All rights reserved.
引用
收藏
页码:1067 / 1071
页数:5
相关论文
共 30 条
[1]  
AJMANI PS, 1999, PHARMAZIE, V54, P3
[2]   The prospects of treatment failure in the chemotherapy of infectious diseases in the 1990s [J].
Armstrong, D ;
Neu, H ;
Peterson, LR ;
Tomasz, A .
MICROBIAL DRUG RESISTANCE-MECHANISMS EPIDEMIOLOGY AND DISEASE, 1995, 1 (01) :1-4
[3]   Synthesis of 25-aminosterols, new antifungal agents [J].
Beuchet, P ;
Dherbomez, M ;
Elkiel, L ;
Charles, G ;
Letourneux, Y .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1999, 9 (11) :1599-1600
[4]   Synthesis of 6(α,β)-aminocholestanols as ergosterol biosynthesis inhibitors [J].
Beuchet, P ;
El kihel, L ;
Dherbomez, M ;
Charles, G ;
Letourneux, Y .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (24) :3627-3630
[5]   Cheno-, urso- and deoxycholic acid spermine conjugates: Relative binding affinities for calf thymus DNA [J].
Blagbrough, IS ;
Al-Hadithi, D ;
Geall, AJ .
TETRAHEDRON, 2000, 56 (21) :3439-3447
[6]   Recent advances in the synthesis of spermine and spermidine analogs of the shark aminosterol squalamine [J].
Brunel, JM ;
Letourneux, Y .
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, 2003, 2003 (20) :3897-3907
[7]  
BRUNEL JM, UNPUB
[8]  
DEICAS E, 1991, MYCOSES, V34, P167, DOI 10.1111/j.1439-0507.1991.tb00638.x
[9]  
El kihel L, 2002, EUR J ORG CHEM, V2002, P4075, DOI 10.1002/1099-0690(200212)2002:23<4075::AID-EJOC4075>3.0.CO
[10]  
2-7