Synthesis and antifungal activity of the novel triazole compounds

WANG Shu-dong; CHEN Xing-dong; ZHAO Qing-jie; ZOU Yan; HU Hong-gang; YU Shi-chong; WANG Ting; CHAI Xiao-yun; REN Hai-xiang

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Objective To design the synthesis and evaluate the antifungal active of the novel triazole compounds based on the structure of fluconazole. Methods The big N,N-disubstituted group was introduced and a series of compounds were synthesized, all of them were confirmed by MS and ¹H NMR, et al. The antifungal activity were also evaluated against the eight common pathogenic fungi. Results Eighteen compounds were synthesized,which exhibited activity against fungi tested. Conclusion The big N,N-disubstituted group introduced to the side chain could affected the antifungal activity.

Synthesis and antifungal activity of the novel triazole compounds

1. The Nanjing General Hospital of Nanjing Military Command, Nanjing 210002, China

2. School of pharmacy, Second Military Medical University, Shanghai, 200433, China

Received Date: 2010-07-07

Rev Recd Date: 2011-03-04

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Abstract: Objective To design the synthesis and evaluate the antifungal active of the novel triazole compounds based on the structure of fluconazole. Methods The big N,N-disubstituted group was introduced and a series of compounds were synthesized, all of them were confirmed by MS and ¹H NMR, et al. The antifungal activity were also evaluated against the eight common pathogenic fungi. Results Eighteen compounds were synthesized,which exhibited activity against fungi tested. Conclusion The big N,N-disubstituted group introduced to the side chain could affected the antifungal activity.

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[1]	Nuccil M, Marr KA. Emerging fungal diseases[J]. Clin Infect Dis, 2005, 41: 521.
[2]	ODDS FC. Resistance of yeasts to azole-derivative antifungals[J]. J Antimicrob Chemother,1993, 31(4): 46.
[3]	Vanden Bossche H, Koymans L, Cytochromes P450 in fungi[J]. Mycoses, 1998,41: (Suppl. l): 32.
[4]	Zhao QJ, Song Y, Hu HG, et al. Design, synthesis and antifungal activity of novel triazole derivatives[J]. Chinese Chemical Letters, 2007, 18: 670.
[5]	Zhao QJ, Hu HG, Li Yw, et al. Design, Synthesis, and antifungal activities of novel 1H-triazole derivatives based on the structure of the active site of fungal lanosterol 14a-demethylase(CYP51)[J]. Chemistry ＆Biodiversity, 2007, 4: 1472.
[6]	Chai XY, Zhang J, Yu SC, et al. Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-y1)-2-(2,4-difluoropheny1)-3-substituted benzylamino-2-propanols[J]. Bioorg Med Chem Lett, 2009, 19(6): 1811.
[7]	章杰兵, 但志刚, 柴晓云, 等. 1-(1H-1,2,4-三唑-1-基)-(2,4-二氟苯基)-3-[N-环丙基-N-(4-取代苄基)]-2-丙醇的合成及抗真菌活性[J]. 药学实践杂志, 2009, 27(2): 107.
[8]	赵庆杰, 宋琰, 胡宏岗, 等. 1-(1H-1,2,4-三唑-1-基)-(2,4-二氟苯基) -3-取代-2-丙醇类化合物的合成及其抗真菌活性[J]. 中国药物化学杂志, 2006, 16(3): 150.
[9]	National committee for clinical laboratory standards. Reference method for broth dilution antifungal susceptibility testing of yeasts,approved standard document M27-A2[S], PA: Wayne: 2002.

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Synthesis and antifungal activity of the novel triazole compounds

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