In vitro activity of 1,3-bisaryloxypropanamines against Trypanosoma cruzi-infected L929 cultures

被引：7
作者：
Lavorato, Stefania Neiva [1 ]
Sales Junior, Policarpo Ademar [2 ]
Fonseca Murta, Silvane Maria [2 ]
Romanha, Alvaro Jose [2 ,3 ]
Alves, Ricardo Jose [1 ]
机构：
[1] Univ Fed Minas Gerais, Fac Farm, Dept Prod Farmaceut, Belo Horizonte, MG, Brazil
[2] Fiocruz MS, Ctr Pesquisas Rene Rachou, Lab Parasitol Celular & Mol, Belo Horizonte, MG, Brazil
[3] Univ Fed Santa Catarina, Dept Microbiol Imunol & Parasitol, Florianopolis, SC, Brazil
来源：
MEMORIAS DO INSTITUTO OSWALDO CRUZ | 2015年 / 110卷 / 04期
关键词：
Trypanosoma cruzi; antitrypanosomal agents; Chagas disease; 1,3-bisaryloxypropanamines; CHAGAS-DISEASE;
D O I：
10.1590/0074-02760150007
中图分类号：
R38 [医学寄生虫学]; Q [生物科学];
学科分类号：
07 ; 0710 ; 09 ; 100103 ;
摘要：
We describe herein the antitrypanosomal activity of 20 novel 1,3-bis(aryloxy)propan-2-amine derivatives. Compounds 2, 4, 6, 12, 15, 16 and 19 were significantly active against amastigote and trypomastigote forms, with half maximal inhibitory concentration values in the range of 6-18 mu M. In the cytotoxicity tests against L929 cells, only compound 4 presented selectivity index value above 10, indicating low toxicity.
引用
收藏
页码：566 / 568
页数：3
相关论文
共 15 条
  • [1] [Anonymous], 2008, QUIMICA MED BASES MO
  • [2] [Anonymous], CHAG DIS
  • [3] Efficient technique for screening drugs for activity against Trypanosoma cruzi using parasites expressing beta-galactosidase
    Buckner, FS
    Verlinde, CLMJ
    LaFlamme, AC
    vanVoorhis, WC
    [J]. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1996, 40 (11) : 2592 - 2597
  • [4] Choi S, 2003, United States patent, Patent No. [US 20030065013 A1, 20030065013]
  • [5] Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors
    de Oliveira, RB
    Vaz, ABM
    Alves, RO
    Liarte, DB
    Donnici, CL
    Romanha, AJ
    Zani, CL
    [J]. MEMORIAS DO INSTITUTO OSWALDO CRUZ, 2006, 101 (02): : 169 - 173
  • [6] New benzylidenethiazolidinediones as antibacterial agents
    Heerding, DA
    Christmann, LT
    Clark, TJ
    Holmes, DJ
    Rittenhouse, SF
    Takata, DT
    Venslavsky, JW
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2003, 13 (21) : 3771 - 3773
  • [7] Trypanocidal activity of lipophilic diamines and amino alcohols
    Junior, C. O. R.
    Alves, R. O.
    Rezende, C. A. M.
    da Costa, C. F.
    Silva, H.
    Le Hyaric, M.
    Fontes, A. P. S.
    Alves, R. J.
    Romanha, A. J.
    de Almeida, M. V.
    [J]. BIOMEDICINE & PHARMACOTHERAPY, 2010, 64 (09) : 624 - 626
  • [8] Update in treatment of Chagas disease
    Le Loup, Guillaume
    Pialoux, Gilles
    Lescure, Francois Xavier
    [J]. CURRENT OPINION IN INFECTIOUS DISEASES, 2011, 24 (05) : 428 - 434
  • [9] Liu YX, 2000, CHINESE J SYNTHETIC, V6, P511
  • [10] In vitro evaluation of the activity of aromatic nitrocompounds against Trypanosoma cruzi
    Oliveira, RB
    Passos, APF
    Alves, RO
    Romanha, AJ
    Prado, MAF
    de Souza, JD
    Alves, RJ
    [J]. MEMORIAS DO INSTITUTO OSWALDO CRUZ, 2003, 98 (01): : 141 - 144
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