NOVEL POLYAMINE DERIVATIVES AS POTENT COMPETITIVE INHIBITORS OF TRYPANOSOMA-CRUZI TRYPANOTHIONE REDUCTASE

被引:27
作者
OSULLIVAN, MC
ZHOU, QB
机构
[1] Department of Chemistry, Indiana State University, Terre Haute
关键词
D O I
10.1016/0960-894X(95)00331-M
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The inhibiting effects of several spermidine and spermine derivatives on I: cruzi trypanothione reductase were assessed. Spermidine and spermine derivatives containing hydrophobic aromatic substituents were found to be competitive inhibitors of trypanothione reductase. The most effective compounds tested were N-1,N-8-bis(2-naphthylmethyl)spermidine, N-4,N-8-bis(2-naphthylmethyl)spermine and N-4,N-8-bis(3-phenylpropyl)spermine.
引用
收藏
页码:1957 / 1960
页数:4
相关论文
共 21 条
  • [1] RATIONALLY DESIGNED SELECTIVE INHIBITORS OF TRYPANOTHIONE REDUCTASE - PHENOTHIAZINES AND RELATED TRICYCLICS AS LEAD STRUCTURES
    BENSON, TJ
    MCKIE, JH
    GARFORTH, J
    BORGES, A
    FAIRLAMB, AH
    DOUGLAS, KT
    [J]. BIOCHEMICAL JOURNAL, 1992, 286 : 9 - 11
  • [2] SYNTHESIS OF N-BENZYLOXYCARBONYL-L-CYSTEINYLGLYCINE 3-DIMETHYLAMINOPROPYLAMIDE DISULFIDE - A CHEAP AND CONVENIENT NEW ASSAY FOR TRYPANOTHIONE REDUCTASE
    ELWAER, A
    DOUGLAS, KT
    SMITH, K
    FAIRLAMB, AH
    [J]. ANALYTICAL BIOCHEMISTRY, 1991, 198 (01) : 212 - 216
  • [3] IDENTIFICATION OF A NOVEL, THIOL-CONTAINING COFACTOR ESSENTIAL FOR GLUTATHIONE-REDUCTASE ENZYME-ACTIVITY IN TRYPANOSOMATIDS
    FAIRLAMB, AH
    CERAMI, A
    [J]. MOLECULAR AND BIOCHEMICAL PARASITOLOGY, 1985, 14 (02) : 187 - 198
  • [4] METABOLISM AND FUNCTIONS OF TRYPANOTHIONE IN THE KINETOPLASTIDA
    FAIRLAMB, AH
    CERAMI, A
    [J]. ANNUAL REVIEW OF MICROBIOLOGY, 1992, 46 : 695 - 729
  • [5] TRYPANOTHIONE - A NOVEL BIS(GLUTATHIONYL)SPERMIDINE COFACTOR FOR GLUTATHIONE-REDUCTASE IN TRYPANOSOMATIDS
    FAIRLAMB, AH
    BLACKBURN, P
    ULRICH, P
    CHAIT, BT
    CERAMI, A
    [J]. SCIENCE, 1985, 227 (4693) : 1485 - 1487
  • [6] FAIRLAMB AH, 1991, BIOCHEM SOC T, V18, P717
  • [7] RATIONAL DESIGN OF PEPTIDE-BASED INHIBITORS OF TRYPANOTHIONE REDUCTASE AS POTENTIAL ANTITRYPANOSOMAL DRUGS
    GARFORTH, J
    MCKIE, JH
    JAOUHARI, R
    BENSON, TJ
    FAIRLAMB, AH
    DOUGLAS, KT
    [J]. AMINO ACIDS, 1994, 6 (03) : 295 - 299
  • [8] SUBVERSIVE SUBSTRATES FOR THE ENZYME TRYPANOTHIONE DISULFIDE REDUCTASE - ALTERNATIVE APPROACH TO CHEMOTHERAPY OF CHAGAS-DISEASE
    HENDERSON, GB
    ULRICH, P
    FAIRLAMB, AH
    ROSENBERG, I
    PEREIRA, M
    SELA, M
    CERAMI, A
    [J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1988, 85 (15) : 5374 - 5378
  • [9] SUBSTRATE-SPECIFICITY OF THE FLAVOPROTEIN TRYPANOTHIONE DISULFIDE REDUCTASE FROM CRITHIDIA-FASCICULATA
    HENDERSON, GB
    FAIRLAMB, AH
    ULRICH, P
    CERAMI, A
    [J]. BIOCHEMISTRY, 1987, 26 (11) : 3023 - 3027
  • [10] IDENTIFICATION AND BIOSYNTHESIS OF N-1,N-9-BIS(GLUTATHIONYL)AMINOPROPYLCADAVERINE (HOMOTRYPANOTHIONE) IN TRYPANOSOMA-CRUZI
    HUNTER, KJ
    LEQUESNE, SA
    FAIRLAMB, AH
    [J]. EUROPEAN JOURNAL OF BIOCHEMISTRY, 1994, 226 (03): : 1019 - 1027