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    
Abstract/OtherAbstract:
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.
Authors:
Shichong Yu; Xiaoyun Chai; Honggang Hu; Yongzheng Yan; Zhongjun Guan; Yan Zou; Qingyan Sun; Qiuye Wu
Related Documents :
14527549 - Solution-phase synthesis of novel delta2-isoxazoline libraries via 1,3-dipolar cycloadd...
19782439 - Stereoselective synthesis and antimicrobial activity of benzofuran-based (1e)-1-(piperi...
20441569 - Derivatization of the azole 1-aminobenzotriazole using laccase of pycnoporus cinnabarin...
20106559 - Synthesis and the selective antifungal activity of 5,6,7,8-tetrahydroimidazo[1,2-a]pyri...
17517449 - Synthesis and antimicrobial studies of novel dichlorofluorophenyl containing aminotriaz...
20036039 - Synthesis, in vitro antibacterial and antifungal evaluations of new alpha-hydroxyphosph...
20121699 - L-ascorbate, a strong inducer of l-dopa (3,4-dihydroxy-l-phenylalanine) production from...
15901159 - Convenient synthesis of nucleoside and isonucleoside analogues.
22559039 - Formation of toxic 2-nonyl-p-benzoquinones from α-tertiary 4-nonylphenol isomers during...
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.
Affiliation:
Department of Organic Chemistry, College of Pharmacy, Second Military Medical University, Guohe Road 325, Shanghai 200433, People's Republic of China.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:
14-alpha Demethylase Inhibitors / chemical synthesis,  chemistry*,  pharmacology*
Antifungal Agents / chemical synthesis,  chemistry*,  pharmacology*
Fungi / drug effects*,  enzymology
Humans
Models, Molecular
Mycoses / drug therapy
Sterol 14-Demethylase / metabolism
Triazoles / chemical synthesis,  chemistry*,  pharmacology*
Chemical
Reg. No./Substance:
0/14-alpha Demethylase Inhibitors; 0/Antifungal Agents; 0/Triazoles; EC 1.14.13.70/Sterol 14-Demethylase

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


Previous Document:  [Handling the therapeutic response from the tumor with PET].
Next Document:  Iodine concentration in cow's milk and its relation with urinary iodine concentrations in the popula...