46708-03-6Relevant articles and documents
Inhibition of Yeast-to-Hypha Transition and Virulence of Candida albicans by 2-Alkylaminoquinoline Derivatives
Meng, Lili,Zhao, He,Zhao, Shuo,Sun, Xiuyun,Zhang, Min,Deng, Yinyue
, (2019)
A rapid increase in Candida albicans infection and drug resistance has caused an emergent need for new clinical strategies against this fungal pathogen. In this study, we evaluated the inhibitory activity of a series of 2-alkylaminoquinoline derivatives against C. albicans isolates. A total of 28 compounds were assessed for their efficacy in inhibiting the yeast-to-hypha transition, which is considered one of the key virulence factors in C. albicans. Several compounds showed strong activity to decrease the morphological transition and virulence of C. albicans cells. The two leading compounds, compound 1 (2-[piperidin-1-yl]quinolone) and compound 12 (6-methyl-2-[piperidin-1-yl]quinoline), remarkably attenuated C. albicans hyphal formation and cytotoxicity in a dose-dependent manner, but they showed no toxicity to either C. albicans cells or human cells. Intriguingly, compound 12 showed an excellent ability to inhibit C. albicans infection in the mouse oral mucosal infection model. This leading compound also interfered with the expression levels of hypha-specific genes in the cyclic AMP-protein kinase A and mitogen-activated protein kinase signaling pathways. Our findings suggest that 2-alkylaminoquinoline derivatives could potentially be developed as novel therapeutic agents against C. albicans infection due to their interference with the yeast-to-hypha transition.
A mild and metal-free synthesis of 2- And 1-alkyl/aryl/dialkyl-aminoquinolines and isoquinolines
Nanaji, Yerramsetti,Kirar, Seema,Pawar, Sandip V.,Yadav, Ashok Kumar
, p. 7628 - 7634 (2020/03/13)
A simple synthetic strategy has been developed for the synthesis of 2- and 1-alkyl/aryl/dialkylaminoquinolines and isoquinolines from the easily available quinoline and isoquinoline-N-oxides, different amines, triflic anhydride as activating agent and ace
2-alkylamine quinoline compound for preventing and treating candida albicans as well as preparation method and application of 2-alkylamine quinoline compound
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Paragraph 0017; 0028; 0029; 0030; 0031, (2018/08/04)
The invention belongs to the technical field of biomedicines and in particular relates to a 2-alkylamine quinoline compound for preventing and treating candida albicans as well as a preparation methodand application of the 2-alkylamine quinoline compound. The compound is prepared from a compound A (1,2,3,4-Tetrahydroquinolines) and a compound B (O-benzoyl hydroxylamines) as raw materials throughsynthesis. Compared with the prior art, the compound has the advantages and effects that results of former research of the inventor show that a diffusible signal factor (DSF) quorum sensing signal anda derivative thereof are capable of relatively intensely interfering conversion of a yeast state to a hypha state of candida albicans, and the compound capable of inhibiting adhesion, hypha state conversion and pathogenicity of the candida albicans is successfully synthesized and screened in the research. Meanwhile, the compound is relatively small in toxicity, growth of the candida albicans andhuman cells is not affected, and the characteristics have the potential of promoting development of novel antifungal drugs.