Document Detail

Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase.
MedLine Citation:
PMID:  20675019     Owner:  NLM     Status:  MEDLINE    
A series of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols (1a-v, 2a-w), which are analogues of fluconazole, have been designed and synthesized as the potential antifungal agents by the click reaction. Click reaction approach toward the synthesis of two sets of novel 1,2,3-triazolyl linked triazole antifungal derivatives 1a-v, 2a-w was achieved by Cu(I)-catalyzed 1,3-dipolar cycloaddition of propargylated intermediate 8 with substituted azidomethyl benzene. The 1,2,3-triazolyl group was inserted into the side chain of the target molecule which can increase the antifungal activity of compounds.
Shichong Yu; Xiaoyun Chai; Honggang Hu; Yongzheng Yan; Zhongjun Guan; Yan Zou; Qingyan Sun; Qiuye Wu
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-08-03
Journal Detail:
Title:  European journal of medicinal chemistry     Volume:  45     ISSN:  1768-3254     ISO Abbreviation:  Eur J Med Chem     Publication Date:  2010 Oct 
Date Detail:
Created Date:  2010-08-30     Completed Date:  2010-12-28     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0420510     Medline TA:  Eur J Med Chem     Country:  France    
Other Details:
Languages:  eng     Pagination:  4435-45     Citation Subset:  IM    
Copyright Information:
Copyright (c) 2010 Elsevier Masson SAS. All rights reserved.
Department of Organic Chemistry, College of Pharmacy, Second Military Medical University, Guohe Road 325, Shanghai 200433, People's Republic of China.
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MeSH Terms
14-alpha Demethylase Inhibitors / chemical synthesis,  chemistry*,  pharmacology*
Antifungal Agents / chemical synthesis,  chemistry*,  pharmacology*
Fungi / drug effects*,  enzymology
Models, Molecular
Mycoses / drug therapy
Sterol 14-Demethylase / metabolism
Triazoles / chemical synthesis,  chemistry*,  pharmacology*
Reg. No./Substance:
0/14-alpha Demethylase Inhibitors; 0/Antifungal Agents; 0/Triazoles; EC 14-Demethylase

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