Synthesis and QSAR studies of some novel disubstituted 1,2,4-triazoles as antimicrobial agents

被引：13
作者：
Panda, Siva S. [1 ]
Jain, Subhash C. [1 ]
机构：
[1] Univ Delhi, Dept Chem, New Delhi 110007, India
来源：
MEDICINAL CHEMISTRY RESEARCH | 2014年 / 23卷 / 02期
关键词：
1,2,4-Triazoles; Quinazoline; Pyridine; Antibacterial; Antifungal; QSAR; IN-VITRO ACTIVITY; ANTIFUNGAL AGENTS; VORICONAZOLE UK-109,496; CANDIDA-ALBICANS; TRIAZOLE; DESIGN; ITRACONAZOLE; COMMON;
D O I：
10.1007/s00044-013-0686-1
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Disubstituted 1,2,4-triazoles 3a-k, 4a-k, and 6a-k have been synthesized from anthranilic acid and nicotinic acid, respectively, through a multi-step reaction sequence via their hydrazides. Synthesized compounds were evaluated for their in vitro antimicrobial activity against two gram-positive bacteria (S. aureus and B. subtilis), three gram-negative bacteria (E. coli, S. typhi, and K. pneumonia) as well as four fungi (A. niger, A. fumigatus, A. flavus, and C. albicans). To explore computational approach, structure-activity relationships were generated statistically using the synthesized compounds and their respective quantitative values of biological activities. These models can be used in future for predicting antimicrobial activity on similar class of compounds.
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收藏
页码：848 / 861
页数：14
相关论文
共 35 条
  • [1] [Anonymous], 2011, MARV 5 6
  • [2] [Anonymous], ARGUSLAB 4 0 1
  • [3] BAILEY EM, 1990, PHARMACOTHERAPY, V10, P146
  • [4] Barry A.L., 1976, ANTIMICROBIC SUSCEPT
  • [5] Quantitative Structure-Activity/Property Relationships: The Ubiquitous Links between Cause and Effect
    Berhanu, Workalemahu M.
    Pillai, Girinath G.
    Oliferenko, Alexander A.
    Katritzky, Alan R.
    [J]. CHEMPLUSCHEM, 2012, 77 (07): : 507 - 517
  • [6] Bossche Hugo Vanden, 1993, Antimicrobial Agents and Chemotherapy, V37, P2101
  • [7] Boyle F T, 1988, Ann N Y Acad Sci, V544, P86, DOI 10.1111/j.1749-6632.1988.tb40391.x
  • [8] Collee J G., 1989, Mackie McCartney practical Medical Microbiology, V13th
  • [9] THE DEVELOPMENT AND USE OF QUANTUM-MECHANICAL MOLECULAR-MODELS .76. AM1 - A NEW GENERAL-PURPOSE QUANTUM-MECHANICAL MOLECULAR-MODEL
    DEWAR, MJS
    ZOEBISCH, EG
    HEALY, EF
    STEWART, JJP
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1985, 107 (13) : 3902 - 3909
  • [10] DOIGNON F, 1992, LETT APPL MICROBIOL, V15, P172, DOI 10.1111/j.1472-765X.1992.tb00755.x
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