Analogues of 4,5-bis(3,5-dichlorophenyl)-2-trifluoromethyl-1H-imidazole as potential antibacterial agents.

被引:184
作者
Antolini, M [1 ]
Bozzoli, A [1 ]
Ghiron, C [1 ]
Kennedy, G [1 ]
Rossi, T [1 ]
Ursini, A [1 ]
机构
[1] GlaxoWellcome SPA, Med Res Ctr, I-37135 Verona, Italy
关键词
D O I
10.1016/S0960-894X(99)00112-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A preliminary exploration of analogues of 4,5-bis(3,5-dichlorophenyl)-2-trifluoromethyl-1H-imidazole, 1, as novel antibacterial agents was carried out to determine the basic features of the structure responsible for the observed biological activity. The presence of two aryl rings, the imidazole NH and either a good electron withdrawing group or an aldehyde or amino group at C-2 were required for good levels of activity against methicillin resistant Staphylococcus aureus (MRSA). (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1023 / 1028
页数:6
相关论文
共 14 条
  • [1] CAVALLERI B, 1977, ARZNEIMITTEL-FORSCH, V27-2, P1889
  • [2] ANTIINFLAMMATORY AND ALDOSE REDUCTASE INHIBITORY ACTIVITY OF SOME TRICYCLIC ARYLACETIC ACIDS
    CERELLI, MJ
    CURTIS, DL
    DUNN, JP
    NELSON, PH
    PEAK, TM
    WATERBURY, LD
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1986, 29 (11) : 2347 - 2351
  • [3] CURTIS NJ, 1980, J ORG CHEM, V45, P4035
  • [4] STEREOCHEMISTRY OF REMOTE DIANION ADDITION TO IMINES - APPLICATION TO THE SYNTHESIS OF (1S, 8AS)-1-HYDROXYINDOLIZIDINE
    GREEN, DLC
    KIDDLE, JJ
    THOMPSON, CM
    [J]. TETRAHEDRON, 1995, 51 (10) : 2865 - 2874
  • [5] ACYL-COA-CHOLESTEROL O-ACYL TRANSFERASE (ACAT) INHIBITORS .1. 2-(ALKYLTHIO)-4,5-DIPHENYL-1H-IMIDAZOLES AS POTENT INHIBITORS OF ACAT
    HARRIS, NV
    SMITH, C
    ASHTON, MJ
    BRIDGE, AW
    BUSH, RC
    COFFEE, ECJ
    DRON, DI
    HARPER, MF
    LYTHGOE, DJ
    NEWTON, CG
    RIDDELL, D
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (23) : 4384 - 4392
  • [6] A NEW AND SELECTIVE METHOD OF OXIDATION
    KORNBLUM, N
    POWERS, JW
    ANDERSON, GJ
    JONES, WJ
    LARSON, HO
    LEVAND, O
    WEAVER, WM
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1957, 79 (24) : 6562 - 6562
  • [7] NEU HC, 1992, SCIENCE, V257, P1073
  • [8] 2-PROTECTING GROUPS FOR 5-LITHIATION IN THE SYNTHESES OF IMIDAZOLES
    NGOCHINDO, RI
    [J]. JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 1990, (06): : 1645 - 1648
  • [9] The renewed challenge of antibacterial chemotherapy
    Niccolai, D
    Tarsi, L
    Thomas, RJ
    [J]. CHEMICAL COMMUNICATIONS, 1997, (24) : 2333 - 2342
  • [10] SEKO N, 1991, CHEM PHARM BULL, V39, P651