Squalamine analogues as potential anti-trypanosomal and anti-leishmanial compounds

被引:25
作者
Khabnadideh, S
Tan, CL
Croft, SL
Kendrick, H
Yardley, V
Gilbert, IH
机构
[1] Univ Wales Coll Cardiff, Welsh Sch Pharm, Cardiff CF10 3XF, S Glam, Wales
[2] Univ London London Sch Hyg & Trop Med, Dept Infect & Trop Med, London WC1E 7HT, England
关键词
D O I
10.1016/S0960-894X(00)00196-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
This paper concerns the synthesis of various simplified analogues of the novel anti-microbial agent, squalamine. The compounds were then investigated for activity against Trypanosoma brucei, the causative agent of African trypanosomiasis, Trypanosoma cruzi, the causative agent of Chagas disease and Leishmania donovani, the causative agent of visceral leishmaniasis. Several compounds showed in vitro activity, especially against T. brucei and L. donovani. However, one compound showed poor in vivo activity, (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1237 / 1239
页数:3
相关论文
共 13 条
  • [1] Squalamine, a novel cationic steroid, specifically inhibits the brush-border Na+/H+ exchanger isoform NHE3
    Akhter, S
    Nath, SK
    Tse, CM
    Williams, J
    Zasloff, M
    Donowitz, M
    [J]. AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY, 1999, 276 (01): : C136 - C144
  • [2] The activities of four anticancer alkyllysophospholipids against Leishmania donovani, Trypanosoma cruzi and Trypanosoma brucei
    Croft, SL
    Snowdon, D
    Yardley, V
    [J]. JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 1996, 38 (06) : 1041 - 1047
  • [3] A synthetic ionophore that recognizes negatively charged phospholipid membranes
    Deng, G
    Dewa, T
    Regen, SL
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1996, 118 (37) : 8975 - 8976
  • [4] The synthesis and characterization of analogs of the antimicrobial compound squalamine: 6 beta-hydroxy-3-aminosterols synthesized from hyodeoxycholic acid
    Jones, SR
    Kinney, WA
    Zhang, XH
    Jones, LM
    Selinsky, BS
    [J]. STEROIDS, 1996, 61 (10) : 565 - 571
  • [5] Antimicrobial activities of squalamine mimics
    Kikuchi, K
    Bernard, EM
    Sadownik, A
    Regen, SL
    Armstrong, D
    [J]. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1997, 41 (07) : 1433 - 1438
  • [6] Sterol-polyamine conjugates as synthetic ionophores
    Merritt, M
    Lanier, M
    Deng, G
    Regen, SL
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1998, 120 (33) : 8494 - 8501
  • [7] SQUALAMINE - AN AMINOSTEROL ANTIBIOTIC FROM THE SHARK
    MOORE, KS
    WEHRLI, S
    RODER, H
    ROGERS, M
    FORREST, JN
    MCCRIMMON, D
    ZASLOFF, M
    [J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1993, 90 (04) : 1354 - 1358
  • [8] SYNTHESIS OF SQUALAMINE - A STEROIDAL ANTIBIOTIC FROM THE SHARK
    MORIARTY, RM
    TULADHAR, SM
    GUO, L
    WEHRLI, S
    [J]. TETRAHEDRON LETTERS, 1994, 35 (44) : 8103 - 8106
  • [9] SYNTHESIS OF 24-XI-SQUALAMINE, AN ANTIINFECTIVE STEROIDAL POLYAMINE
    PECHULIS, AD
    BELLEVUE, FH
    CIOFFI, CL
    TRAPP, SG
    FOJTIK, JP
    MCKITTY, AA
    KINNEY, WA
    FRYE, LL
    [J]. JOURNAL OF ORGANIC CHEMISTRY, 1995, 60 (16) : 5121 - 5126
  • [10] RAPID CONSTRUCTION OF A SQUALAMINE MIMIC
    SADOWNIK, A
    DENG, G
    JANOUT, V
    REGEN, SL
    BERNARD, EM
    KIKUCHI, K
    ARMSTRONG, D
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1995, 117 (22) : 6138 - 6139