scholarly journals An engineered biosynthetic–synthetic platform for production of halogenated indolmycin antibiotics

2021 ◽  
Author(s):  
Elesha R. Hoffarth ◽  
Sunnie Kong ◽  
Hai-Yan He ◽  
Katherine S. Ryan
Keyword(s):  
Staphylococcus Aureus ◽  
Methicillin Resistant ◽  
Derivatives Of

A semi-synthetic system for producing indolmycin, an antibiotic, was developed and used to make indole-substituted, halogenated derivatives of indolmycin, some with modest bioactivity against methicillin-resistant Staphylococcus aureus.

scholarly journals Synthesis and biological evaluation of truncated derivatives of abyssomicin C as antibacterial agents

2019 ◽  
Vol 15 ◽  
pp. 1468-1474
Author(s):  
Leticia Monjas ◽  
Peter Fodran ◽  
Johanna Kollback ◽  
Carlo Cassani ◽  
Thomas Olsson ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Natural Product ◽  
Antibacterial Agents ◽  
Biological Evaluation ◽  
Methicillin Resistant ◽  
Structure Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of ◽  
Novel Antibiotics

The synthesis and antibacterial activity of two new highly truncated derivatives of the natural product abyssomicin C are reported. This work outlines the limits of structural truncation of the natural product and consequently provides insights for further structure–activity relationship studies towards novel antibiotics targeting 4-amino-4-deoxychorismate (ADC) synthase. Specifically, it is demonstrated that the synthetically challenging bicyclic motif is essential for activity towards methicillin-resistant Staphylococcus aureus (MRSA).

scholarly journals Prodrugs of Cephalosporin RWJ-333441 (MC-04,546) with Improved Aqueous Solubility

2003 ◽  
Vol 47 (6) ◽  
pp. 2043-2046 ◽  
Author(s):  
Scott J. Hecker ◽  
Trevor Calkins ◽  
Mary E. Price ◽  
Keith Huie ◽  
Sharon Chen ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Aqueous Solubility ◽  
Amino Group ◽  
Methicillin Resistant ◽  
Ph Values ◽  
Primary Amino ◽  
Derivatives Of ◽  
Acyl Derivatives

ABSTRACT To improve the aqueous solubility of anti-methicillin-resistant Staphylococcus aureus cephalosporin RWJ-333441 for parenteral administration, acyl derivatives of the C-3 primary amino group were prepared and evaluated for solubility, cleavage in serum in vitro, and conversion to RWJ-333441 in vivo. Improved solubility at physiologic pH values and release of RWJ-333441 in vitro and in vivo were observed for several prodrugs, including the aspartate derivative RWJ-333442.

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