Synthesis, antifungal and antibacterial activity of novel 1,2,4-triazole derivatives

被引:61
作者
Gupta, Deepa [1 ]
Jain, D. K. [2 ]
机构
[1] LBS Coll Pharm, Dept Pharm, Jaipur, Rajasthan, India
[2] IPS Coll Pharm, Dept Pharm, Indore, Madhya Pradesh, India
关键词
Antibacterial activity; antifungal activity; Microsporum gypseum; Schiff bases; Staphylococcus aureus;
D O I
10.4103/2231-4040.161515
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
A large number of 1,2,4-triazole-containing ring system have been incorporated into a wide variety of therapeutically interesting drug candidates including anti-inflammatory, central nervous system stimulants, antianxiety, and antimicrobial agents. To overcome the rapid development of drug resistance, new agents should preferably have chemical characteristics that clearly differ from those of existing agents. Thus led to the design and synthesize the new antimicrobial agents. A novel series of Schiff bases based on of 4-(benzylideneamino)-5-phenyl-4H-1,2,4-triazole-3-thiol scaffold was prepared by heating thiocarbohydrazide and substituted benzoic acid and subsequently, treating with substituted benzaldehydes. Seventeen derivatives were synthesized and were biologically screened for antifungal and antibacterial activity. The newly synthesized derivatives of triazole showed antifungal activity against fungal species, Microsporum gypseum; and antibacterial activity against bacterial species, Staphylococcus aureus. It was observed that none of the compounds tested showed positive results for fungi Candida albicans fungi Aspergillus niger, nor against bacterial strain Escherichia coli. Strong antifungal effects were obtained for the synthesized compounds against M. gypseum and were superior or comparable to standard drug ketoconazole. Similarly, all of the synthesized compounds exhibit strong antibacterial activity against S. aureus and were superior or comparable to standard drug streptomycin. It was found that among the triazole derivatives so synthesized, six of them, showed antifungal activity superior to ketoconazole while one of them, showed antibacterial activity superior to streptomycin. Thus, these can be the potential new molecule as an antimicrobial agent.
引用
收藏
页码:141 / 146
页数:6
相关论文
共 50 条
  • [21] Synthesis and antimicrobial activities of novel quinoline derivatives carrying 1,2,4-triazole moiety
    Eswaran, Sumesh
    Adhikari, Airody Vasudeva
    Shetty, N. Suchetha
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (11) : 4637 - 4647
  • [22] Antimicrobial activity of novel substituted 1,2,4-triazole and 1,3-thiazole derivatives
    Saffour, Sana
    AL-Sharabi, Amal A.
    Evren, Asaf Evrim
    Cankilic, Meral Yilmaz
    Yurttas, Leyla
    JOURNAL OF MOLECULAR STRUCTURE, 2024, 1295
  • [23] Microwave Assistant Synthesis, Antifungal Activity and DFT Theoretical Study of Some Novel 1,2,4-Triazole Derivatives Containing Pyridine Moiety
    Sun, Guo-Xiang
    Yang, Ming-Yan
    Shi, Yan-Xia
    Sun, Zhao-Hui
    Liu, Xing-Hai
    Wu, Hong-Ke
    Li, Bao-Ju
    Zhang, Yong-Gang
    INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 2014, 15 (05) : 8075 - 8090
  • [24] Synthesis and anti-inflammatory properties of novel 1,2,4-triazole derivatives
    El-Serwy, Walaa S.
    Mohamed, Neama A.
    Abbas, Eman M.
    Abdel-Rahman, Rehab F.
    RESEARCH ON CHEMICAL INTERMEDIATES, 2013, 39 (06) : 2543 - 2554
  • [25] Synthesis and Biological Activity of 1H-1,2,4-Triazole Alcohol Derivatives
    Liu, Jianbing
    Dai, Hong
    Liu, Wei
    Fang, Jianxin
    SYNTHESIS AND REACTIVITY IN INORGANIC METAL-ORGANIC AND NANO-METAL CHEMISTRY, 2008, 38 (08) : 647 - 651
  • [26] Synthesis, antifungal and antibacterial evaluation of trifluoromethylpyrimidine derivatives containing 1,3,4-thiadiazole and 1,2,4-triazole thioether moieties
    An, Jian-Song
    Hu, Shu-Hui
    Chen, Hai-Jiang
    Fei, Qiang
    Wu, Wen-Neng
    PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS, 2025, : 372 - 382
  • [27] Synthesis and Herbicidal Activity of 1,2,4-Triazole Derivatives Containing a Pyrazole Moiety
    Mu, Jin-Xia
    Zhai, Zhi-Wen
    Tan, Cheng-Xia
    Weng, Jian-Quan
    Wu, Hong-Ke
    Duke, Stephen O.
    Zhang, Yong-Gang
    Liu, Xing-Hai
    JOURNAL OF HETEROCYCLIC CHEMISTRY, 2019, 56 (03) : 968 - 971
  • [28] Microwave-Assisted Synthesis and Antifungal Activity of Some Novel Thioethers Containing 1,2,4-Triazole Moiety
    Min, Li-Jing
    Shi, Yan-Xia
    Wu, Hong-Ke
    Sun, Zhao-Hui
    Liu, Xing-Hai
    Li, Bao-Ju
    Zhang, Yong-Gang
    APPLIED SCIENCES-BASEL, 2015, 5 (04): : 1211 - 1220
  • [29] Design, Synthesis, and Bioactivity Evaluation of Novel Sulfone Derivatives Incorporating an 1,2,4-Triazole Moiety
    Liu, J.
    He, C.
    Tan, B.
    Wu, W.
    Yu, L.
    Li, P.
    RUSSIAN JOURNAL OF GENERAL CHEMISTRY, 2025, 95 (03) : 757 - 763
  • [30] Synthesis and antimicrobial evaluation of novel 1,2,4-triazole thioether derivatives bearing a quinazoline moiety
    Fan, Zhijiang
    Shi, Jun
    Bao, Xiaoping
    MOLECULAR DIVERSITY, 2018, 22 (03) : 657 - 667