scholarly journals Synthesis and biological evaluation of 1,2-disubsubstituted 4-quinolone analogues ofPseudonocardiasp. natural products

2018 ◽  
Vol 14 ◽  
pp. 2680-2688
Author(s):  
Stephen M Geddis ◽  
Teodora Coroama ◽  
Suzanne Forrest ◽  
James T Hodgkinson ◽  
Martin Welch ◽  
...  
Keyword(s):  
Natural Products ◽  
Total Synthesis ◽  
Bacterial Species ◽  
Biological Evaluation ◽  
Human Pathogen ◽  
Growth Defects ◽  
Structure Activity ◽  
Related Series ◽  
Relationship Of ◽  
Synthesis And Biological Evaluation

A series of analogues ofPseudonocardiasp. natural products were synthesized, which have been reported to possess potent antibacterial activity againstHelicobacter pyloriand induce growth defects inEscherichia coliandStaphylococcus aureus. Taking inspiration from a methodology used in our total synthesis of natural products, we applied this methodology to access analogues possessing bulky N-substituents, traditionally considered to be challenging scaffolds. Screening of the library provided valuable insights into the structure–activity relationship of the bacterial growth defects, and suggested that selectivity between bacterial species should be attainable. Furthermore, a structurally related series of analogues was observed to inhibit production of the virulence factor pyocyanin in the human pathogenPseudomonas aeruginosa, which may be a result of their similarity to thePseudomonasquinolone signal (PQS) quorum sensing autoinducer. This provided new insights regarding the effect of N-substitution in PQS analogues, which has been hitherto underexplored.

scholarly journals Total Synthesis and Biological Evaluation of Phaeosphaerides

Catalysts ◽  
2018 ◽  
Vol 8 (5) ◽  
pp. 206 ◽  
Author(s):  
Kenichi Kobayashi ◽  
Kosaku Tanaka ◽  
Hiroshi Kogen
Keyword(s):  
Crystal Structure ◽  
Natural Products ◽  
Total Synthesis ◽  
Structure Analysis ◽  
Endophytic Fungus ◽  
Biological Evaluation ◽  
Crystal Structure Analysis ◽  
X Ray ◽  
Structure Activity ◽  
Synthesis And Biological Evaluation

This article reviews studies regarding the total synthesis of phaeosphaerides A and B, nitrogen-containing bicyclic natural products isolated from an endophytic fungus. Numerous synthetic efforts and an X-ray crystal structure analysis of phaeosphaeride A have enabled revision of its originally proposed structure. In addition, a successful protic acid-mediated transformation of phaeosphaeride A to phaeosphaeride B revealed the hypothetical biosynthesis of phaeosphaeride B from phaeosphaeride A. Structure–activity relationship studies of phaeosphaeride derivatives are also discussed.

Total synthesis and biological evaluation of ustiloxin natural products and two analogs

2006 ◽  
Vol 16 (18) ◽  
pp. 4804-4807 ◽  
Author(s):  
Pixu Li ◽  
Cory D. Evans ◽  
Erin M. Forbeck ◽  
Haengsoon Park ◽  
Ruoli Bai ◽  
...  
Keyword(s):  
Natural Products ◽  
Total Synthesis ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

Total Synthesis and Biological Evaluation of the Resveratrol-Derived Polyphenol Natural Products Hopeanol and Hopeahainol A

2010 ◽  
Vol 132 (21) ◽  
pp. 7540-7548 ◽  
Author(s):  
K. C. Nicolaou ◽  
Qiang Kang ◽  
T. Robert Wu ◽  
Chek Shik Lim ◽  
David Y.-K. Chen
Keyword(s):  
Natural Products ◽  
Total Synthesis ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

Design, synthesis and biological evaluation of novel peptide MC2 analogues from Momordica charantia as potential anti-diabetic agents

2015 ◽  
Vol 13 (15) ◽  
pp. 4551-4561 ◽  
Author(s):  
Baowei Yang ◽  
Xue Li ◽  
Chenyu Zhang ◽  
Sijia Yan ◽  
Wei Wei ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Biological Evaluation ◽  
Momordica Charantia ◽  
Activity Relationship ◽  
Design Synthesis ◽  
Structure Activity ◽  
Oxidative Effects ◽  
Relationship Of ◽  
Synthesis And Biological Evaluation

The structure–activity relationship of peptide MC2 resulted in the development of compoundIII-3, which exhibited potent anti-hyperglycaemic and anti-oxidative effects.

Total Synthesis and Biological Evaluation of Ustiloxin Natural Products and Two Analogues.

ChemInform ◽  
2007 ◽  
Vol 38 (1) ◽  
Author(s):  
Pixu Li ◽  
Cory D. Evans ◽  
Erin M. Forbeck ◽  
Haengsoon Park ◽  
Ruoli Bai ◽  
...  
Keyword(s):  
Natural Products ◽  
Total Synthesis ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

The antimitotic Podophyllotoxin and its derivatives- recent synthetic advances

2021 ◽  
Vol 02 ◽  
Author(s):  
Sharon Riaz ◽  
Khalid Mohammed Khan ◽  
Ghayoor Abbas Chotana ◽  
Amir Faisal ◽  
Rahman Shah Zaib Saleem
Keyword(s):  
Total Synthesis ◽  
Chemical Space ◽  
Structural Features ◽  
Biological Evaluation ◽  
One Pot ◽  
Antimitotic Activity ◽  
Structure Activity ◽  
Synthetic Approaches ◽  
Podophyllotoxin Derivatives ◽  
Synthesis And Biological Evaluation

: The substantial antimitotic potential of podophyllotoxin and its derivatives has attracted both synthetic and medicinal chemists to expand the chemical space for the subsequent biological evaluation of these compounds. The interest ranges from total synthesis, hemi-synthesis, one-pot synthetic approaches and structure-activity relationship studies. In the first segment of the review, we present recent development in the synthesis of podophyllotoxin and also describe its mode of action. The second section covers the synthesis and the structure-activity relationships of podophyllotoxin derivatives, along with the discussion of important structural features required by the molecule for displaying antimitotic activity. The last part describes the synthesis and biological evaluation of potent 4-aza podophyllotoxin derivatives. This review is of interest to chemists who study natural and synthetic compounds for drug discovery.

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