Medetomidine Analogs as α2-Adrenergic Ligands. 3. Synthesis and Biological Evaluation of a New Series of Medetomidine Analogs and Their Potential Binding Interactions with α2-Adrenoceptors Involving a “Methyl Pocket”

1997 ◽  
Vol 40 (19) ◽  
pp. 3014-3024 ◽  
Author(s):  
Xiaoyan Zhang ◽  
Joseph E. De Los Angeles ◽  
Mei-Ying He ◽  
James T. Dalton ◽  
Gamal Shams ◽  
...  

Planta Medica ◽  
2013 ◽  
Vol 79 (05) ◽  
Author(s):  
PR Polepally ◽  
BL Roth ◽  
K White ◽  
E Vardy ◽  
JK Zjawiony




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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