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 ◽  
...  

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).

2020 ◽  
Vol 11 (6) ◽  
pp. 5257-5265
Author(s):  
Samia Rabah ◽  
Kahina Kouachi ◽  
Patrícia A. B. Ramos ◽  
Ana Peixoto Gomes ◽  
Adelaide Almeida ◽  
...  

Allium triquetrum L. bulbs, flowers and leaves are proved to be valuable sources of value-added lipophilic compounds, specifically as antibacterial agents against methicillin-resistant Staphylococcus aureus.


Synlett ◽  
2020 ◽  
Vol 31 (05) ◽  
pp. 475-481
Author(s):  
Stavroula A. Zisopoulou ◽  
Spyridon Bousis ◽  
Jörg Haupenthal ◽  
Jennifer Herrmann ◽  
Rolf Müller ◽  
...  

A library of novel 2-substituted derivatives of the antibiotic natural product pentenomycin I is presented. The new collection of analogues is divided in two main classes, 2-alkynyl- and 2-aryl- derivatives, which are accessed by the appropriate type of palladium-catalyzed cross-coupling reaction of the 2-iodo-protected pentenomycin I with suitable nucleophiles. The new derivatives were tested for their activity against certain types of bacteria and one of them, compound 8h, was found to exhibit significant inhibitory activity against several Gram-positive bacteria but also displayed cytotoxic activity against eukaryotic cell lines.


2021 ◽  
Author(s):  
Qin Zhang ◽  
Yan-Shi Xiong ◽  
Jianxin Chen ◽  
Yanhui Tan ◽  
Xiangwen Liao ◽  
...  

Abstract Four new ruthenium (II) polypyridine complexes bearing 18β-glycyrtinic acid derivatives, [Ru(bpy)2L](PF6)2 (Ru1), [Ru(dmb)2L](PF6)2 (Ru2), [Ru(dtb)2L](PF6)2 (Ru3) and [Ru(phen)2L](PF6)2 (Ru4) (bpy = 2,2-bipyridine, dmb = 4,4'-dimethyl-2,2'-bipyridine, dtb = 4,4'-di-tert-butyl-2,2'-bipyridine, phen...


2015 ◽  
Vol 13 (28) ◽  
pp. 7720-7735 ◽  
Author(s):  
Takeshi Nakaya ◽  
Akira Matsuda ◽  
Satoshi Ichikawa

Caprazamycin analogues, which were designed and synthesized via an aza-Prins–Ritter reaction, exhibit a good MraY and antibacterial activity without cytotoxicity against human cells.


Coumarin is a heterocyclic moiety containing benzo pyran ring structure. It is widely distributed in the plant kingdom as a glycoside. Many compounds of medicinal and pharmaceutical importance possess coumarin ring structure. Drugs with coumarin structure can be synthesized by many well-known synthetic reactions. Coumarin derivatives were found to be antibacterial, anticoagulant, antiinflammatory, anti-HIV, anti-cancer and antioxidant. As part of the search for new and effective antibacterial agents, eight novel derivatives of coumarins were synthesized by Mannich reaction. All the compounds were evaluated for antibacterial activity against Staphylococcus aureus and Escherichia coli using ciprofloxacin as standard and DMSO as solvent. Three of the synthesized derivatives exhibited good antibacterial activity against Staphylococcus aureus and Escherichia coli. The work must be extended so as to develop coumarin derivatives into highly effective antibacterial agents.


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