Syntheses of novel antimycobacterial combinatorial libraries of structurally diverse substituted pyrimidines by three-component solid-phase reactions

被引:58
作者
Kumar, A
Sinha, S
Chauhan, PMS [1 ]
机构
[1] Cent Drug Res Inst, Div Med Chem, Lucknow 226001, Uttar Pradesh, India
[2] Cent Drug Res Inst, Div Biochem, Lucknow 226001, Uttar Pradesh, India
关键词
D O I
10.1016/S0960-894X(01)00829-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A new pyrimidine based scaffold has been developed by three-component solid-phase syntheses. The utility of scaffolds was demonstrated by synthesizing libraries of 80 substituted pyrimidines 12(a-p), 13(a p), 14(a p), 15(la-p), 16(a-p). Among 80 compounds screened, six compounds, 12i, 13c, 14d, 14e, 14o, and 15d showed in vitro activity against Mycobacterium tuberculosis (MABA) at a concentration of 50 and 25 mug/mL. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:667 / 669
页数:3
相关论文
共 28 条
  • [1] Novel antiallergic agents. Part I: Synthesis and pharmacology of pyrimidine amide derivatives
    Ban, M
    Taguchi, H
    Katsushima, T
    Aoki, S
    Watanabe, A
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY, 1998, 6 (07) : 1057 - 1067
  • [2] Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity
    Barbachyn, MR
    Hutchinson, DK
    Brickner, SJ
    Cynamon, MH
    Kilburn, JO
    Klemens, SP
    Glickman, SE
    Grega, KC
    Hendges, SK
    Toops, DS
    Ford, CW
    Zurenko, GE
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (03) : 680 - 685
  • [3] TUBERCULOSIS IN PATIENTS WITH HUMAN-IMMUNODEFICIENCY-VIRUS INFECTION
    BARNES, PF
    BLOCH, AB
    DAVIDSON, PT
    SNIDER, DE
    [J]. NEW ENGLAND JOURNAL OF MEDICINE, 1991, 324 (23) : 1644 - 1650
  • [4] NATIONWIDE SURVEY OF DRUG-RESISTANT TUBERCULOSIS IN THE UNITED-STATES
    BLOCH, AB
    CAUTHEN, GM
    ONORATO, IM
    DANSBURY, KG
    KELLY, GD
    DRIVER, CR
    SNIDER, DE
    [J]. JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION, 1994, 271 (09): : 665 - 671
  • [5] TUBERCULOSIS - COMMENTARY ON A REEMERGENT KILLER
    BLOOM, BR
    MURRAY, CJL
    [J]. SCIENCE, 1992, 257 (5073) : 1055 - 1064
  • [6] CHAUHAN PMS, 1994, INDIAN J CHEM B, V33, P32
  • [7] CHAUHAN PMS, IN PRESS COMBIN CHEM
  • [8] Drug-resistant tuberculosis: Review of the worldwide situation and the WHO/IUATLD global surveillance project
    Cohn, DL
    Bustreo, F
    Raviglione, MC
    [J]. CLINICAL INFECTIOUS DISEASES, 1997, 24 : S121 - S130
  • [9] 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
  • [10] FINE PEM, 1994, TUBERCULOSIS BACK FU, P53