Design, synthesis, and antifungal activities of novel triazole derivatives containing the benzyl group

被引：30

作者：

Xu, Kehan ^{[1
]}

Huang, Lei ^{[1
]}

Xu, Zheng ^{[2
]}

Wang, Yanwei ^{[1
,3
]}

Bai, Guojing ^{[1
]}

Wu, Qiuye ^{[1
]}

Wang, Xiaoyan ^{[1
]}

Yu, Shichong ^{[1
]}

Jiang, Yuanying ^{[1
]}

机构：

[1] Second Mil Med Univ, Sch Pharm, Shanghai 200433, Peoples R China

[2] Second Mil Med Univ, Shanghai Changzheng Hosp, Shanghai 200433, Peoples R China

[3] 422 Hosp PLA, Zhanjiang, Peoples R China

来源：

DRUG DESIGN DEVELOPMENT AND THERAPY | 2015年 / 9卷

基金：

中国国家自然科学基金;

关键词：

triazole; synthesis; antifungal activity; CYP51; MOLECULAR DOCKING; AGENTS; RESISTANCE; THERAPY; ITRACONAZOLE; MECHANISMS; DRUGS;

D O I：

10.2147/DDDT.S74989

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In previous studies undertaken by our group, a series of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols (1a-r), which were analogs of fluconazole, was designed and synthesized by click chemistry. In the study reported here, the in vitro antifungal activities of all the target compounds were evaluated against eight human pathogenic fungi. Compounds 1a, 1q, and 1r showed the more antifungal activity than the others.

引用

页码：1459 / 1467

页数：9

共 29 条

[1]

[Anonymous], 2002, M27A2 NAT COMM CLIN

[2]

[Anonymous], 2010, EUR J MED CHEM, DOI DOI 10.1016/j.ejmech.2010.07.002

[3] Antifungal agents.: 11.: N-substituted derivatives of 1-[(aryl)(4-aryl-1H-pyrrol-3-yl)methyl]-1H-imidazole:: Synthesis, anti-Candida activity, and QSAR studies [J].

Di Santo, R ;

Tafi, A ;

Costi, R ;

Botta, M ;

Artico, M ;

Corelli, F ;

Forte, M ;

Caporuscio, F ;

Angiolella, L ;

Palamara, AT .

JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (16) :5140-5153

[4] Epidemiology of nosocomial fungal infections [J].

Fridkin, SK ;

Jarvis, WR .

CLINICAL MICROBIOLOGY REVIEWS, 1996, 9 (04) :499-&

[5]

Gadhave P. P., 2010, Annals of Biological Research, V1, P82

[6] Antifungals: mechanism of action and resistance, established and novel drugs [J].

Georgopapadakou, NH .

CURRENT OPINION IN MICROBIOLOGY, 1998, 1 (05) :547-557

[7] Antifungal agents: Mode of action, mechanisms of resistance, and correlation of these mechanisms with bacterial resistance [J].

Ghannoum, MA ;

Rice, LB .

CLINICAL MICROBIOLOGY REVIEWS, 1999, 12 (04) :501-+

[8]

Groll Andreas H, 2012, Future Microbiol, V7, P179, DOI 10.2217/fmb.11.154

[9] Systemic mycoses in the immunocompromised host: an update in antifungal therapy [J].

Kontoyiannis, DP ;

Mantadakis, E ;

Samonis, G .

JOURNAL OF HOSPITAL INFECTION, 2003, 53 (04) :243-258

[10] Biodiversity of CYP51 in trypanosomes [J].

Lepesheva, G. I. ;

Hargrove, T. Y. ;

Ott, R. D. ;

Nes, W. D. ;

Waterman, M. R. .

BIOCHEMICAL SOCIETY TRANSACTIONS, 2006, 34 :1161-1164

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