Substituted 4-methylquinolines as a new class of anti-tuberculosis agents

被引:73
作者
Jain, R [1 ]
Vaitilingam, B [1 ]
Nayyar, A [1 ]
Palde, PB [1 ]
机构
[1] Natl Inst Pharmaceut Educ & Res, Dept Med Chem, SAS Nagar 160062, Punjab, India
关键词
D O I
10.1016/S0960-894X(03)00074-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
We report synthesis and anti-tuberculosis activities of a series of novel ring-substituted quinolines. The most effective compound of the series 3d (MIC = 6.25 mug/mL, Mycobacterium tuberculosis H37 Rv strain) was synthesized in one step; thus is an attractive lead molecule for anti-tuberculosis drug development. The results of this study represent the discovery of ring-substituted 4-methylquinolines as new class of potential anti-tuberculosis agents. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1051 / 1054
页数:4
相关论文
共 21 条
  • [1] SILVER(I)-CATALYZED OXIDATIVE DECARBOXYLATION OF ACIDS BY PEROXYDISULFATE - ROLE OF SILVER(II)
    ANDERSON, JM
    KOCHI, JK
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1970, 92 (06) : 1651 - &
  • [2] Microplate Alamar blue assay versus BACTEC 460 system for high-throughput screening of compounds against Mycobacterium tuberculosis and Mycobacterium avium
    Collins, LA
    Franzblau, SG
    [J]. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1997, 41 (05) : 1004 - 1009
  • [3] DAVID S, 1996, TUBERCULOSIS
  • [4] Duncan K, 1997, CHEM IND-LONDON, P861
  • [5] Rapid, low-technology MIC determination with clinical Mycobacterium tuberculosis isolates by using the microplate Alamar Blue assay
    Franzblau, SG
    Witzig, RS
    McLaughlin, JC
    Torres, P
    Madico, G
    Hernandez, A
    Degnan, MT
    Cook, MB
    Quenzer, VK
    Ferguson, RM
    Gilman, RH
    [J]. JOURNAL OF CLINICAL MICROBIOLOGY, 1998, 36 (02) : 362 - 366
  • [6] A GENERAL, SELECTIVE, AND CONVENIENT PROCEDURE OF HOMOLYTIC FORMYLATION OF HETEROAROMATIC BASES
    GIORDANO, C
    MINISCI, F
    VISMARA, E
    LEVI, S
    [J]. JOURNAL OF ORGANIC CHEMISTRY, 1986, 51 (04) : 536 - 537
  • [7] Synthesis of novel ring-substituted histidines and histamines
    Jain, R
    Cohen, LA
    King, MM
    [J]. TETRAHEDRON, 1997, 53 (13) : 4539 - 4548
  • [8] Regiospecific alkylation of histidine and histamine at C-2
    Jain, R
    Cohen, LA
    ElKadi, NA
    King, MM
    [J]. TETRAHEDRON, 1997, 53 (07) : 2365 - 2370
  • [9] KEN D, 1997, J PHARM PHARMACOL, V49, P1
  • [10] McConnell J, 1998, LANCET, V351, P852