Synthesis and Biological Evaluation of Nipecotic Acid and Guvacine Derived 1,3‐Disubstituted Allenes as Inhibitors of Murine GABA Transporter mGAT1

ChemMedChem ◽  
2019 ◽  
Vol 14 (12) ◽  
pp. 1135-1151 ◽  
Author(s):  
Maren Schaarschmidt ◽  
Georg Höfner ◽  
Klaus T. Wanner
Keyword(s):  
Biological Evaluation ◽  
Gaba Transporter ◽  
Nipecotic Acid ◽  
Synthesis And Biological Evaluation

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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