23468-00-0Relevant academic research and scientific papers
Nickel-catalyzed sonogashira reactions of non-activated secondary alkyl bromides and iodides
Yi, Jun,Lu, Xi,Sun, Yan-Yan,Xiao, Bin,Liu, Lei
supporting information, p. 12409 - 12413 (2013/12/04)
A nicked reaction: The title reaction of terminal alkynes with non-activated secondary alkyl iodides and bromides was accomplished for the first time. This reaction provides a new and practical approach for the synthesis of substituted alkynes (see scheme; cod=cyclo-1,5-octadiene). Copyright
Synthesis and biological evaluation of vinyl ether-containing azole derivatives as inhibitors of Trichophyton rubrum
Wang, Lulu,Yang, Wenge,Wang, Kai,Zhu, Jing,Shen, Fei,Hu, Yonghong
scheme or table, p. 4887 - 4890 (2012/08/07)
In an attempt to search for many target compounds with excellent activities, a series of vinyl ether-containing azole derivatives were designed, synthesized, and evaluated as antifungal agents. Results of preliminary antifungal tests against Trichophyton rubrum in vitro indicated that most of the synthesized compounds showed excellent activities. In comparison with fluconazole, itraconazole, voriconazole, omoconazole and amphotericin B, several compounds (such as 7d, 7g and 7h) exhibited more potent inhibitory activities, suggesting that they were promising leads for the development of novel antifungal agents.
ANTIFUNGAL 1, 2, 4-TRIAZOLYL DERIVATIVES
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Page/Page column 116, (2010/12/31)
The present invention relates to novel triazole compounds of the formulae (I), (II) and (IV) as defined below, to agricultural and pharmaceutical compositions containing them and to their use as fungicides, antimycotic, anticancer and antiviral agents.
Discovery of highly potent novel antifungal azoles by structure-based rational design
Wang, Wenya,Sheng, Chunquan,Che, Xiaoying,Ji, Haitao,Cao, Yongbing,Miao, Zhenyuan,Yao, Jianzhong,Zhang, Wannian
supporting information; experimental part, p. 5965 - 5969 (2010/07/04)
On the basis of the active site of lanosterol 14α-demethylase from Candida albicans (CACYP51), a series of new azoles were designed and synthesized. All the new azoles show excellent in vitro activity against most of the tested pathogenic fungi, which represent a class of promising leads for the development of novel antifungal agents. The MIC80 value of compounds 8c, 8i and 8n against C. albicans is 0.001 μg/mL, indicating that these compounds are more potent than fluconazole, itraconazole and voriconazole. Flexible molecular docking was used to analyze the structure-activity relationships (SARs) of the compounds. The designed compounds interact with CACYP51 through hydrophobic, van der Waals and hydrogen-bonding interactions.
Synthesis and antidepressant activity of substituted (ω-Aminoalkoxy)benzene derivatives
Kikumoto,Tobe,Tonomura
, p. 145 - 148 (2007/10/02)
A series of substituted (ω-aminoalkoxy)benzene derivatives has been synthesized and screened for potential antidepressant activities. The effect of structural variation of these molecules has been systematically examined. Antidepressant activity was clearly displayed by 2-benzyl-1-[4-(methylamino)butoxy]benzene (7), 2-(2-hydroxybenzyl)-1-[4(methylamino)butoxy]benzene (19), 1-[4-(methylamino)butoxy]-2-phenoxybenzene (29), and 1-[4-(methylamino)butoxy]-2-(phenylthio)benzene (31) in further pharmacological studies. These compounds did not possess the anticholinergic, antihistaminic, and muscle-relaxant side effects common to tricyclic antidepressants.
