Synthesis and biological evaluation of novel 1,2,3-benzotriazin-4-one derivatives as leukotriene A 4 hydrolase aminopeptidase inhibitors

2017 ◽  
Vol 28 (5) ◽  
pp. 1044-1048 ◽  
Author(s):  
Fan Zhang ◽  
Dang Wu ◽  
Gao-Lei Wang ◽  
Shuang Hou ◽  
Ping Ou-Yang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Aminopeptidase Inhibitors

Synthesis and Biological Evaluation of the Antimicrobial Natural Product Lipoxazolidinone A

2018 ◽  
Author(s):  
Jonathan J. Mills ◽  
Kaylib R. Robinson ◽  
Troy E. Zehnder ◽  
Joshua G. Pierce
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Mechanism Of Action ◽  
Marine Natural Products ◽  
Biological Evaluation ◽  
Lead Compounds ◽  
Follow Up Studies ◽  
Initial Resistance ◽  
Synthesis And Biological Evaluation

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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