scholarly journals Advancements in the synthesis of fused tetracyclic quinoline derivatives

RSC Advances ◽  
2020 ◽  
Vol 10 (34) ◽  
pp. 19867-19935 ◽  
Author(s):  
Ramadan A. Mekheimer ◽  
Mariam A. Al-Sheikh ◽  
Hanadi Y. Medrasi ◽  
Kamal U. Sadek
Keyword(s):  
Natural Products ◽  
Wide Spectrum ◽  
Biological Properties ◽  
Quinoline Derivatives ◽  
Important Class ◽  
Bioactive Natural Products

Fused tetracyclic systems containing a quinoline nucleus represent an important class of heterocyclic bioactive natural products and pharmaceuticals because of their significant and wide-spectrum biological properties.

scholarly journals An Alternative Approach towards C-12 Functionalized Scalaranic Sesterterpenoids. Synthesis of 17-Oxo-20-norscalaran-12α,19-O-lactone

Marine Drugs ◽  
2021 ◽  
Vol 19 (11) ◽  
pp. 636
Author(s):  
Olga Morarescu ◽  
Marina Grinco ◽  
Veaceslav Kulciţki ◽  
Sergiu Shova ◽  
Nicon Ungur
Keyword(s):  
Functional Groups ◽  
Aldol Condensation ◽  
Wide Spectrum ◽  
Condensation Reaction ◽  
Diffraction Method ◽  
Biological Properties ◽  
Marine Sponges ◽  
X Ray Diffraction ◽  
Bioactive Natural Products ◽  
Oxygenated Functional Groups

Scalarane sesterterpenoids emerged as interesting bioactive natural products which were isolated extensively from marine sponges and shell-less mollusks. Some representatives were also reported recently from superior plants. Many scalarane sesterterpenoids displayed a wide spectrum of valuable properties, such as antifeedant, antimicrobial, antifungal, antitubercular, antitumor, anti-HIV properties, cytotoxicity and stimulation of nerve growth factor synthesis, as well as anti-inflammatory activity. Due to their important biological properties, many efforts have been undertaken towards the chemical synthesis of natural scalaranes. The main synthetic challenges are connected to their complex polycyclic framework, chiral centers and different functional groups, in particular the oxygenated functional groups at the C-12 position, which are prerequisites of the biological activity of many investigated scalaranes. The current work addresses this problem and the synthesis of 17-oxo-20-norscalaran-12α,19-O-lactone is described. It was performed via the 12α-hydroxy-ent-isocopal-13(14)-en-15-al obtained from (-)-sclareol as an accessible starting material. The tetracyclic lactone framework was built following an addition strategy, which includes the intramolecular Michael addition of a diterpenic acetoacetic ester and an intramolecular aldol condensation reaction as key synthetic steps. The structure and stereochemistry of the target compound have been proven by X-Ray diffraction method.

scholarly journals Lignans

Molecules ◽  
2019 ◽  
Vol 24 (7) ◽  
pp. 1424 ◽  
Author(s):  
David Barker
Keyword(s):  
Natural Products ◽  
Research Articles ◽  
Important Class ◽  
Special Issue ◽  
Bioactive Natural Products

The 13 research articles/communications, six reviews, and one perspective that comprise this Special Issue on Lignans, highlight the most recent research and investigations into this diverse and important class of bioactive natural products [...]

scholarly journals De Novo Peptide Sequencing Reveals a Vast Cyclopeptidome in Human Gut and Other Environments

2019 ◽  
Author(s):  
Bahar Behsaz ◽  
Hosein Mohimani ◽  
Alexey Gurevich ◽  
Andrey Prjibelski ◽  
Mark F. Fisher ◽  
...  
Keyword(s):  
Natural Products ◽  
Gastrointestinal Tract ◽  
Cyclic Peptides ◽  
De Novo ◽  
Genome Mining ◽  
Human Microbiome ◽  
Important Class ◽  
Human Gastrointestinal Tract ◽  
Human Gut ◽  
Bioactive Natural Products

ABSTRACTCyclic and branch cyclic peptides (cyclopeptides) represent an important class of bioactive natural products that include many antibiotics and anti-tumor compounds. However, little is known about cyclopeptides in the human gut, despite the fact that humans are constantly exposed to them. To address this bottleneck, we developed the CycloNovo algorithm for de novo cyclopeptide sequencing that employs de Bruijn graphs, the workhorse of DNA sequencing algorithms. CycloNovo reconstructed many new cyclopeptides that we validated with transcriptome, metagenome, and genome mining analyses. Our benchmarking revealed a vast hidden cyclopeptidome in the human gut and other environments and suggested that CycloNovo offers a much-needed step-change for cyclopeptide discovery. Furthermore, CycloNovo revealed a wealth of anti-microbial cyclopeptides from food that survive the complete human gastrointestinal tract, raising the question of how these cyclopeptides might affect the human microbiome.SIGNIFICANCEThe golden age of antibiotics was followed by a decline in the pace of antibiotics discovery in the 1990s. The key prerequisite for the resurgence of antibiotics research is the development of a computational discovery pipeline for antibiotics sequencing. We describe such pipeline for cyclic and branch cyclic peptides (cyclopeptides) that represent an important class of bioactive natural products such as antibiotics and anti-tumor compounds. Our CycloNovo algorithm for cyclopeptide sequencing reconstructed many new cyclopeptides that we validated with transcriptome, metagenome, and genome mining analyses. CycloNovo revealed a wealth of anti-microbial cyclopeptides from food that survive the complete human gastrointestinal tract, raising the question of how these cyclopeptides might affect the human microbiome.

scholarly journals Natural Products from the Marine Sponge Subgenus Reniera

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1097
Author(s):  
Xuelian Bai ◽  
Yang Liu ◽  
Hao Wang ◽  
Huawei Zhang
Keyword(s):  
Natural Products ◽  
Therapeutic Potential ◽  
Chemical Study ◽  
Biological Properties ◽  
Marine Sponges ◽  
Extensive Literature ◽  
Lead Discovery ◽  
Bioactive Natural Products ◽  
Drug Lead ◽  
Extensive Literature Search

Marine sponges are one of the prolific producers of bioactive natural products with therapeutic potential. As an important subgenus of Haliclona, Reniera sponges are mainly distributed in the Mediterranean Sea and Atlantic area, and had been chemically investigated for over four decades. By an extensive literature search, this review first makes a comprehensive summary of all natural products from Reniera sponges and their endozoic microbes, as well as biological properties. Perspectives on strengthening the chemical study of Reniera sponges for new drug-lead discovery are provided in this work.

Biotransformations of Bioactive Natural Products with Complicated Structures

Planta Medica ◽  
2012 ◽  
Vol 78 (05) ◽  
Author(s):  
JG Dai ◽  
RD Chen ◽  
D Xie ◽  
JH Li ◽  
K Wang ◽  
...  
Keyword(s):  
Natural Products ◽  
Bioactive Natural Products

Diverse chemical and biological potentials of various pyridazine and pyridazinone derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
Industrial Chemical ◽  
Anti Inflammatory ◽  
Pyridazinone Derivatives

A series of heterocyclic compounds incorporating pyridazine moiety were for diverse biological activities. Pyridazines and pyridazinones derivatives showed wide spectrum of biological activities such as vasodialator, cardiotonic, anticonvulsant, antihypertensive, antimicrobial, anti-inflammatory, analgesic, anti-feedant, herbicidal, and various other biological, agrochemical and industrial chemical activities. The results illustrated that the synthesized pyridazine/pyridazine compounds have diverse and significant biological activities. Mechanistic insights into the biological properties of pyridazinone derivatives and various synthetic techniques used for their synthesis are also described.

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