261959-40-4Relevant articles and documents
Synthesis and bioactivity evaluation of novel azoles containing dithiocarbamate moieties
Fu, Ben,Wu, Maocheng,Huang, Lu,Wu, Qiuye,Wang, Shudong,Chai, Xiaoyun
, p. 2491 - 2498 (2017)
A series of novel azoles, N-methyl-N-[2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)]-propyl-(1-substituted phenyl)-dithiocarbamate has been designed, synthesized, and screened for antifungal activity by minimum inhibitory concentration. Results of preliminary antifungal tests showed that most of the title compounds had good antifungal activities against nearly all the tested fungal pathogens, especially against the Candida species. The most surprising finding of this study is that compound 4a, 4e, and 4k exhibited higher activities than fluconazole against Aspergillus fumigatus.
A sulfur-containing [...] fungal compound and its preparation and use
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Paragraph 0034; 0035, (2016/11/07)
The invention is a sulfur/nitrogen-containing azole antifungal compound as well as a preparation method and an application of the sulfur/nitrogen-containing azole antifungal compound, relates to the technical field of medicine. The sulfur/nitrogen-containing azole antifungal compound is a novel azole antifungal compound and has a chemical structural formula which is shown in the specification, wherein, R1 is hydrogen or a straight-chain or branched-chain saturated or unsaturated lower alkyl having 1-6 carbon atoms; R2 is selected from hydrogen, alkyl, halogen, cyano group, a nitro group, an amino and an alkoxy, can be located at the ortho, meta or para position of the benzene ring and can be monosubstituted or polysubstituted. The invention also provides a preparation method and an application of the compound. The compound disclosed by the invention has strong antifungal activity on the deep fungal, has the advantages of high efficiency, low toxicity, broad anti-fungal spectrum and the like compared with the current clinically applied antifungal drugs, and therefore, the compound can be used for the preparation of efficient antifungal agents.
Synthesis and antifungal activity of the novel triazole compounds
Yu, Shichong,Chai, Xiaoyun,Wang, Nan,Cui, Hong,Zhao, Qingjie,Hu, Honggang,Zou, Yan,Sun, Qingyan,Wu, Qiuye
, p. 704 - 708 (2013/06/05)
A series of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-substituted- 2-propanols (1a-o) which are analogues of fluconazole, have been designed and synthesized for the first time by the click reaction on the basis of computational docking experiments to the active site of the cytochrome P450 14α-demethylase (CYP51). Their structures were characterized by 1H NMR, 13C NMR and HRMS. The in vitro antifungal activities of all the target compounds were evaluated against eight human pathogenic fungi.
Design of new antifungal agents: synthesis and evaluation of 1-[(1H-indol-5-ylmethyl)amino]-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan- 2-ols
Guillon, Remi,Giraud, Francis,Loge, Cedric,Le Borgne, Marc,Picot, Carine,Pagniez, Fabrice,Le Pape, Patrice
scheme or table, p. 5833 - 5836 (2010/04/28)
We previously reported on the design and synthesis of 1-[((hetero)aryl- or piperidinylmethyl)amino]-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols showing various degrees of antifungal activity against Candida albicans and Aspergillus fumigatus strains. N