Synthesis and structure-activity relationships of some 2,5-disubstituted benzoxazoles and benzimidazoles as antimicrobial agents

被引:0
|
作者
Sener, E
Yalcin, I
Temiz, O
Oren, I
Akin, A
Ucarturk, N
机构
[1] ANKARA UNIV,FAC PHARM,DEPT PHARMACEUT CHEM,TR-06100 TANDOGAN,ANKARA,TURKEY
[2] ANKARA UNIV,FAC PHARM,DEPT MICROBIOL,TR-06100 TANDOGAN,ANKARA,TURKEY
来源
FARMACO | 1997年 / 52卷 / 02期
关键词
D O I
暂无
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The synthesis of a new series of 2,5-disubstitutedbenzoxazoles 5a-e, and 2,5-disubstitutedbenzimidazoles 6a-h are described in order to determine their antimicrobial activities and feasible structure-activity relationships (SAR). The synthesized compounds were tested in vitro against 3 Gram-positive, 3 Gram-negative, bacteria and a fungus Candida albicans. 5c, and 5e were found most active than the others against Bacillus subtilis at a MIC value of 3.12 mu g/ml and the compounds 5e, 6a and 6e indicated significant antibacterial activity against the enterobacter Pseudomonas aeruginosae. 5a, 5c, 5d and 6d also exhibited antimycotic activity against C. albicans. The antibacterial and antimycotic activities of 5-6 are compared with several control drugs.
引用
收藏
页码:99 / 103
页数:5
相关论文
共 50 条
  • [41] STEREOSELECTIVITY IN THE SYNTHESIS OF 2,5-DISUBSTITUTED PYRROLIDINES
    KINSMAN, R
    LATHBURY, D
    VERNON, P
    GALLAGHER, T
    JOURNAL OF THE CHEMICAL SOCIETY-CHEMICAL COMMUNICATIONS, 1987, (04) : 243 - 244
  • [42] A NEW SYNTHESIS OF 2,5-DISUBSTITUTED PYRIDINES
    GIAM, CS
    STOUT, JL
    JOURNAL OF THE CHEMICAL SOCIETY D-CHEMICAL COMMUNICATIONS, 1970, (08): : 478 - &
  • [43] NEW SYNTHESIS OF 2,5-DISUBSTITUTED THIOPHENES
    SMUTNY, EJ
    JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1969, 91 (01) : 208 - &
  • [44] SYNTHESIS AND STRUCTURE ACTIVITY RELATIONSHIP OF 2,5-DISUBSTITUTED THIOPHENE DERIVATIVES FOR β-AMYLOID PLAQUE IMAGING
    Chandra, R.
    Kung, M. -P.
    Kung, H. F.
    JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2005, 48 : S167 - S167
  • [45] SYNTHESIS OF 3,5-DISUBSTITUTED PYRIDINES AS ANTIMICROBIAL AGENTS
    ATTIA, A
    ABOGHALIA, MH
    ELSALAM, OIA
    PHARMAZIE, 1995, 50 (07): : 455 - 459
  • [46] SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF SOME NOVEL 2,5-DISUBSTITUTED 1,3,4-THIADIAZOLES FOR THEIR POTENTIAL ANTIMICROBIAL ACTIVITY
    Rajak, H.
    Veerasamy, R.
    Gupta, A. Kumar
    Kharya, M. Dhar
    Mishra, P.
    DIGEST JOURNAL OF NANOMATERIALS AND BIOSTRUCTURES, 2009, 4 (03) : 443 - 451
  • [47] SEARCH FOR ANTICHOLINERGIC AGENTS .35. DETERMINATION OF STRUCTURE-ACTIVITY RELATIONSHIP IN NOVEL 2,5-DISUBSTITUTED 1,3-DIOXANE DERIVATIVES
    ILCZUK, A
    ACTA POLONIAE PHARMACEUTICA, 1982, 39 (5-6): : 337 - 343
  • [48] Identification and structure-activity relationships of 2,6-disubstituted pyrazines as antituberculosis agents
    Sun, Yongmao
    Petukhova, Valentina
    Giri, Rajan S.
    Klein, Larry L.
    Song, Yang
    Zhang, Nan
    Peng, Kuan Wei
    Wan, Baojie
    Wang, Yuehong
    Franzblau, Scott G.
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2010, 240
  • [49] Structure-Activity Relationships of 1,2-Disubstituted Benzimidazoles: Selective Inhibition of Heme Oxygenase-2 Activity
    Kong, Xianqi
    Vukomanovic, Dragic
    Nakatsu, Kanji
    Szarek, Walter A.
    CHEMMEDCHEM, 2015, 10 (08) : 1435 - 1441
  • [50] THE SYNTHESIS AND LIQUID-CRYSTAL PROPERTIES OF SOME 2,5-DISUBSTITUTED PYRIDINES
    BURROW, MP
    GRAY, GW
    LACEY, D
    TOYNE, KJ
    LIQUID CRYSTALS, 1988, 3 (12) : 1643 - 1653