Synthesis and Biological Evaluation of gem-Diamine 1-N-Iminosugars Related to L-Iduronic Acid as Inhibitors of Heparan Sulfate 2-O-Sulfotransferase.

ChemInform ◽  
2006 ◽  
Vol 37 (18) ◽  
Author(s):  
Jillian R. Brown ◽  
Yoshio Nishimura ◽  
Jeffrey D. Esko
Keyword(s):  
Heparan Sulfate ◽  
Biological Evaluation ◽  
Iduronic Acid ◽  
Synthesis And Biological Evaluation

Convergent chemoenzymatic synthesis and biological evaluation of a heparan sulfate proteoglycan syndecan-1 mimetic

2021 ◽  
Vol 57 (27) ◽  
pp. 3407-3410
Author(s):  
Jia Gao ◽  
Yongmei Xu ◽  
Jian Liu ◽  
Xuefei Huang
Keyword(s):  
Heparan Sulfate ◽  
Biological Evaluation ◽  
Heparan Sulfate Proteoglycan ◽  
Chemoenzymatic Synthesis ◽  
Sulfate Proteoglycan ◽  
Biological Studies ◽  
Synthesis Strategy ◽  
Synthesis And Biological Evaluation

A new convergent chemoenzymatic synthesis strategy has been established to efficiently synthesize a mimetic of structurally well-defined heparan sulfate proteoglycan syndecan-1 glyco-polypeptide at a milligram scale to enable biological studies.

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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