scholarly journals Synthesis and biological evaluation of quinolone derivatives as transthyretin amyloidogenesis inhibitors and fluorescence sensors

2022 ◽  
Vol 53 ◽  
pp. 116550
Author(s):  
Ah Reum Han ◽  
Eun Hee Jeon ◽  
Kun Woo Kim ◽  
Seul Ki Lee ◽  
Chan-yeong Ohn ◽  
...  
RSC Advances ◽  
2018 ◽  
Vol 8 (30) ◽  
pp. 16494-16502 ◽  
Author(s):  
Xuan Wang ◽  
Xiaoye Jiang ◽  
Shiyou Sun ◽  
Yongqiong Liu

Synthesis of a series of novel dual-acting levofloxacin–HDACi conjugates, which show potent inhibitory activities against HDACs, tubulin polymerization, and significant antiproliferative effect on MCF-7 cells.


2018 ◽  
Author(s):  
Jonathan J. Mills ◽  
Kaylib R. Robinson ◽  
Troy E. Zehnder ◽  
Joshua G. Pierce

The lipoxazolidinone family of marine natural products, with an unusual 4-oxazolidinone heterocycle at their core, represents a new scaffold for antimicrobial discovery; however, questions regarding their mechanism of action and high lipophilicity have likely slowed follow-up studies. Herein, we report the first synthesis of lipoxazolidinone A, 15 structural analogs to explore its active pharmacophore, and initial resistance and mechanism of action studies. These results suggest that 4-oxazolidinones are valuable scaffolds for antimicrobial development and reveal simplified lead compounds for further optimization.


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