In Pursuit of Natural Product Leads: Synthesis and Biological Evaluation of 2-[3-hydroxy-2-[(3-hydroxypyridine-2-carbonyl)amino]phenyl]benzoxazole-4-carboxylic acid (A-33853) and Its Analogues: Discovery ofN-(2-Benzoxazol-2-ylphenyl)benzamides as Novel Antileishmanial Chemotypes

2008 ◽  
Vol 51 (23) ◽  
pp. 7344-7347 ◽  
Author(s):  
Suresh K. Tipparaju ◽  
Sipak Joyasawal ◽  
Marco Pieroni ◽  
Marcel Kaiser ◽  
Reto Brun ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Natural Product ◽  
Biological Evaluation ◽  
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.

scholarly journals Synthesis and Biological Evaluation of New Heteroaryl Carboxylic Acid Derivatives as Anti-inflammatory-Analgesic Agents

2013 ◽  
Vol 61 (2) ◽  
pp. 222-228 ◽  
Author(s):  
Khaled Abouzid Mohamed Abouzid ◽  
Nadia Abdalla Khalil ◽  
Eman Mohamed Ahmed ◽  
Sawsan Abo-Bakr Zaitone
Keyword(s):  
Carboxylic Acid ◽  
Biological Evaluation ◽  
Analgesic Agents ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation

Synthesis and biological evaluation of acylated oligorhamnoside derivatives structurally related to mezzettiaside-6 with cytotoxic activity

2016 ◽  
Vol 14 (28) ◽  
pp. 6691-6702 ◽  
Author(s):  
Gaopeng Song ◽  
Sumei Li ◽  
Zhiwei Lei ◽  
Yibin Li ◽  
Junhua Li ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Natural Product ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

Two partially acylated oligorhamnoside derivatives 1 and 2 structurally related to the natural product mezzettiaside-6 were synthesized via a ‘2 + 1 + 1’ convergent strategy.

Total synthesis and biological evaluation of the natural product (−)-cyclonerodiol, a new inhibitor of IL-4 signaling

2014 ◽  
Vol 12 (47) ◽  
pp. 9707-9715 ◽  
Author(s):  
Jens Langhanki ◽  
Kristina Rudolph ◽  
Gerhard Erkel ◽  
Till Opatz
Keyword(s):  
Total Synthesis ◽  
Natural Product ◽  
Specific Inhibitor ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

The sesquiterpene (−)-cyclonerodiol is a specific inhibitor of IL-4 induced STAT6 signaling and is readily available from (−)-linalool.

scholarly journals Synthesis and Biological Evaluation of Novel 2-Substituted ­Analogues of (–)-Pentenomycin I

Synlett ◽  
2020 ◽  
Vol 31 (05) ◽  
pp. 475-481
Author(s):  
Stavroula A. Zisopoulou ◽  
Spyridon Bousis ◽  
Jörg Haupenthal ◽  
Jennifer Herrmann ◽  
Rolf Müller ◽  
...  
Keyword(s):  
Natural Product ◽  
Coupling Reaction ◽  
Cross Coupling ◽  
Eukaryotic Cell ◽  
Biological Evaluation ◽  
Gram Positive Bacteria ◽  
Cross Coupling Reaction ◽  
Palladium Catalyzed ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

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.

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