Design, Microwave-Assisted Synthesis and in Vitro Antibacterial and Antifungal Activity of 2,5-Disubstituted Benzimidazole

被引:17
|
作者
Shi, Yanpeng [1 ]
Jiang, Kai [2 ]
Zheng, Ran [1 ]
Fu, Jiaxu [1 ]
Yan, Liuqing [1 ]
Gu, Qiang [1 ]
Zhang, Yumin [1 ]
Lin, Feng [2 ]
机构
[1] Jilin Univ, Coll Chem, Changchun 130012, Jilin, Peoples R China
[2] Jilin Univ, Sch Life Sci, Changchun 130012, Jilin, Peoples R China
关键词
2,5-disubstituted benzimidazole; microwave-assisted synthesis; antimicrobial activity; biological activity; synthesis design; RESISTANT STAPHYLOCOCCUS-EPIDERMIDIS; ANTIMICROBIAL ACTIVITY; CANDIDA-ALBICANS; DERIVATIVES; AUREUS; INHIBITORS; INFECTION; EFFICIENT; THERAPY;
D O I
10.1002/cbdv.201800510
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Seventeen novel 2,5-disubstituted benzimidazole derivatives were designed, synthesized and evaluated for their antibacterial activities. The tested compounds B1-B4 and C2-C6 exhibited not only good antifungal activity but also favorable broad-spectrum antibacterial activity. Also, the lowest MIC of antibacterial and antifungal activity was 2 mu g/mL and 4 mu g/mL, respectively. It suggested that the structure of compound including the different substituent and its sites directly affected the efficacy of the synthesized compounds.
引用
收藏
页数:11
相关论文
共 50 条
  • [21] A NEW SYNTHESIS OF 2,5-DISUBSTITUTED PYRIDINES
    GIAM, CS
    STOUT, JL
    JOURNAL OF THE CHEMICAL SOCIETY D-CHEMICAL COMMUNICATIONS, 1970, (08): : 478 - &
  • [22] 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
  • [23] NEW SYNTHESIS OF 2,5-DISUBSTITUTED THIOPHENES
    SMUTNY, EJ
    JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1969, 91 (01) : 208 - &
  • [24] Microwave-assisted synthesis of new benzimidazole derivatives with lipase inhibition activity
    Mentese, Emre
    Bektas, Hakan
    Ulker, Serdar
    Bekircan, Olcay
    Kahveci, Bahittin
    JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2014, 29 (01) : 64 - 68
  • [25] Microwave-Assisted Synthesis of Some New Benzimidazole Derivatives with their Antimicrobial Activity
    Mentese, Emre
    Yilmaz, Fatih
    Beris, Fatih Saban
    Bekircan, Olcay
    Kahveci, Bahittin
    CURRENT MICROWAVE CHEMISTRY, 2015, 2 (01) : 32 - 39
  • [26] Conventional and microwave-assisted synthesis of pyrazole derivatives and screening of their antibacterial and antifungal activities
    Mistry, B. D.
    Desai, K. R.
    Patel, J. A.
    Patel, N. I.
    INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY, 2012, 51 (05): : 746 - 751
  • [27] Synthesis of 3,5-disubstituted isoxazolines as potential antibacterial and antifungal agents
    Imran, M
    Khan, SA
    INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY, 2004, 13 (03) : 213 - 216
  • [28] Synthesis and antifungal activity of novel 2,5-disubstituted-1,3,4-oxadiazoles containing benzimidazole moiety
    Zhang, Zeyuan
    Mu, Wei
    Ji, Zengchen
    Jiang, Lin
    JOURNAL OF PESTICIDE SCIENCE, 2012, 37 (04) : 338 - 341
  • [29] Conventional and Microwave-Assisted Synthesis of Benzimidazole Derivatives and Their In Vitro Inhibition of Human Cyclooxygenase
    Secci, Daniela
    Bolasco, Adriana
    D'Ascenzio, Melissa
    della Sala, Flavio
    Yanez, Matilde
    Carradori, Simone
    JOURNAL OF HETEROCYCLIC CHEMISTRY, 2012, 49 (05) : 1187 - 1195
  • [30] Microwave assisted one-pot synthesis of some 2,5-disubstituted 1,3,4-oxadiazoles
    Kalluraya, B.
    Rao, Jyothi N.
    Sujith, K. V.
    INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY, 2008, 17 (04) : 359 - 362