PANG Tao, WU Mao-cheng, WANG Xiao-yi. Synthesis and antifungal activities of new triazole compounds[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(5): 373-376. doi: 10.3969/j.issn.1006-0111.2013.05.016
Citation:
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PANG Tao, WU Mao-cheng, WANG Xiao-yi. Synthesis and antifungal activities of new triazole compounds[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(5): 373-376. doi: 10.3969/j.issn.1006-0111.2013.05.016
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Synthesis and antifungal activities of new triazole compounds
- 1.
Department of pharmacy, Changzheng Hospital, Second Military Medical University, Shanghai 200003, China
- 2.
Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
- 3.
College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306, China
- Received Date: 2013-03-12
- Rev Recd Date:
2013-04-28
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Abstract
Objective To design and synthesis novel triazole antifungal derivatives and study the antifungal activity. Methods All the target compounds were prepared from 1,3-difluorobenzene via click reaction;The antibacterial activities of the title compounds were determined with broth dilution method. Results Twelve compounds were synthesized and characterized by 1H NMR and MS. All the title compounds exhibited potent antifungal activities against nearly all fungi tested. Conclusion The electronic effects of the substituents affected the activity of compounds, specifically the electron-donating groups.
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References
[1]
|
熊建琼,邓朝霞,张 雷,等. 伊曲康唑在多器官功能障碍综合征患者侵袭性真菌感染中的应用[J].第三军医大学学报, 2006, 28 (11):1260. |
[2]
|
Kontoyiannis DP,Sagar N,Hirschi KD,et al. Overexpression of Erg11p by the regulatable GAL1 promoter confers fluconazole resistance in Saccharomyces cerevisiae[J]. Antimicrob Agents Chemother, 1999, 43(11): 2798. |
[3]
|
季海涛,张万年,周有骏.抗真菌药物作用靶点羊毛甾醇14α-去甲基化酶研究[J].生物化学与生物物理进展,1999,26(2):108. |
[4]
|
Phempel M. Experiences, recognitions and questions in azole antimycotics[J]. Jpn J Med Mycol, 1982, 23(1): 17. |
[5]
|
Jiang Y,Zhang J,Cao Y,et al. Synthesis, in vitro evaluation and molecular docking studies of new triazole derivatives as antifungal agents[J]. Bioorg Med Chem Lett,2011, 21(15): 4471. |
[6]
|
Chai X,Zhang J,Cao Y,et al. Design, synthesis and molecular docking studies of novel triazole as antifungal agent[J]. Eur J Med Chem,2011, 46(7): 3167. |
[7]
|
Kolb HC,Finn MG,Sharpless KB,et al. Click chemistry: diverse chemical function from a few good reactions[J]. Angew Chem Int Ed, 2001, 40(11): 2004. |
[8]
|
Pore VS,Aher NG,Kumar M,et al. Design and synthesis of fluconazole-bile acid conjugate using cick reaction[J]. Tetrahedron 2006, 62: 11178. |
[9]
|
National Committee for Clinical Laboratory Standards.Reference method for broth dilution antifungal susceptibility testing of yeasts approved standard[S]. Document M27-A2, Wayne, PA, 2002. |
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Proportional views
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