Marine AChE inhibitors isolated from Geodia barretti: natural compounds and their synthetic analogs

2016 ◽  
Vol 14 (5) ◽  
pp. 1629-1640 ◽  
Author(s):  
Elisabeth K. Olsen ◽  
Espen Hansen ◽  
Lindon W. K. Moodie ◽  
Johan Isaksson ◽  
Kristina Sepčić ◽  
...  
Keyword(s):  
Natural Compounds ◽  
Synthetic Analogs ◽  
Ache Inhibitors ◽  
Electric Eel

Barettin, 8,9-dihydrobarettin, bromoconicamin and a novel brominated marine indole were isolated from Geodia barretti and evaluated as inhibitors of electric eel acetylcholinesterase together with synthetic analogs.

ChemInform Abstract: Marine AChE Inhibitors Isolated from Geodia barretti: Natural Compounds and Their Synthetic Analogues.

ChemInform ◽  
2016 ◽  
Vol 47 (24) ◽  
Author(s):  
Elisabeth K. Olsen ◽  
Espen Hansen ◽  
Lindon W. K. Moodie ◽  
Johan Isaksson ◽  
Kristina Sepcic ◽  
...  
Keyword(s):  
Natural Compounds ◽  
Synthetic Analogues ◽  
Ache Inhibitors

scholarly journals Synthesis of 4-O-Alkylated N-Acetylneuraminic Acid Derivatives

2020 ◽  
Author(s):  
Emil Johansson ◽  
Rémi Caraballo ◽  
Mikael Elofsson
Keyword(s):  
Drug Discovery ◽  
Mammalian Cells ◽  
Natural Compounds ◽  
Neuraminic Acid ◽  
Synthetic Analogs ◽  
Acetylneuraminic Acid ◽  
Health And Disease ◽  
Alkylation Reactions

<p><i>N</i>-acetyl neuraminic acid<i> </i>(Neu5Ac) is a densely functionalized nine-carbon monosaccharide. It ubiquitously decorates the surface of mammalian cells were it is found in terminal positions of glycolipids and glycoproteins. This important saccharide and natural analogs play important roles in a number of processes in health and disease. Despite this few Neu5Ac based therapeutics have been developed. To further study and understand the chemistry and biology of Neu5Ac efficient protocols for synthesis of the parent natural compounds as well as synthetic analogs are required. In the manuscript, we report investigation of alkylation reactions to produce selectively modified Neu5Ac with focus on position 4. The study provides insights in the reaction and we establish robust protocols that allow selective modification of Neu5Ac for use as tool compounds and starting points for drug discovery.</p>

scholarly journals Synthesis of 4-O-Alkylated N-Acetylneuraminic Acid Derivatives

2020 ◽  
Author(s):  
Emil Johansson ◽  
Rémi Caraballo ◽  
Mikael Elofsson
Keyword(s):  
Drug Discovery ◽  
Mammalian Cells ◽  
Natural Compounds ◽  
Neuraminic Acid ◽  
Synthetic Analogs ◽  
Acetylneuraminic Acid ◽  
Health And Disease ◽  
Alkylation Reactions

<p><i>N</i>-acetyl neuraminic acid<i> </i>(Neu5Ac) is a densely functionalized nine-carbon monosaccharide. It ubiquitously decorates the surface of mammalian cells were it is found in terminal positions of glycolipids and glycoproteins. This important saccharide and natural analogs play important roles in a number of processes in health and disease. Despite this few Neu5Ac based therapeutics have been developed. To further study and understand the chemistry and biology of Neu5Ac efficient protocols for synthesis of the parent natural compounds as well as synthetic analogs are required. In the manuscript, we report investigation of alkylation reactions to produce selectively modified Neu5Ac with focus on position 4. The study provides insights in the reaction and we establish robust protocols that allow selective modification of Neu5Ac for use as tool compounds and starting points for drug discovery.</p>

scholarly journals Potential Therapeutic Approaches to Alzheimer’s Disease By Bioinformatics, Cheminformatics And Predicted Adme-Tox Tools

2020 ◽  
Vol 18 (8) ◽  
pp. 696-719
Author(s):  
Speranta Avram ◽  
Maria Mernea ◽  
Carmen Limban ◽  
Florin Borcan ◽  
Carmen Chifiriuc
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Nmda Receptors ◽  
In Silico ◽  
Molecular Mechanisms ◽  
Neurodegenerative Disorder ◽  
Experimental Studies ◽  
Natural Compounds ◽  
Synthetic Compounds ◽  
Ache Inhibitors

Background: Alzheimer’s disease (AD) is considered a severe, irreversible and progressive neurodegenerative disorder. Currently, the pharmacological management of AD is based on a few clinically approved acethylcholinesterase (AChE) and N-methyl-D-aspartate (NMDA) receptor ligands, with unclear molecular mechanisms and severe side effects. Methods: Here, we reviewed the most recent bioinformatics, cheminformatics (SAR, drug design, molecular docking, friendly databases, ADME-Tox) and experimental data on relevant structurebiological activity relationships and molecular mechanisms of some natural and synthetic compounds with possible anti-AD effects (inhibitors of AChE, NMDA receptors, beta-secretase, amyloid beta (Aβ), redox metals) or acting on multiple AD targets at once. We considered: (i) in silico supported by experimental studies regarding the pharmacological potential of natural compounds as resveratrol, natural alkaloids, flavonoids isolated from various plants and donepezil, galantamine, rivastagmine and memantine derivatives, (ii) the most important pharmacokinetic descriptors of natural compounds in comparison with donepezil, memantine and galantamine. Results: In silico and experimental methods applied to synthetic compounds led to the identification of new AChE inhibitors, NMDA antagonists, multipotent hybrids targeting different AD processes and metal-organic compounds acting as Aβ inhibitors. Natural compounds appear as multipotent agents, acting on several AD pathways: cholinesterases, NMDA receptors, secretases or Aβ, but their efficiency in vivo and their correct dosage should be determined. Conclusion: Bioinformatics, cheminformatics and ADME-Tox methods can be very helpful in the quest for an effective anti-AD treatment, allowing the identification of novel drugs, enhancing the druggability of molecular targets and providing a deeper understanding of AD pathological mechanisms.

Dexamethasone Effect on Embryonic Chick Respiratory Epithelium

1982 ◽  
Vol 40 ◽  
pp. 248-249
Author(s):  
M.R. Richter ◽  
R.V. Blystone
Keyword(s):  
Lung Development ◽  
Critical Role ◽  
Respiratory Epithelium ◽  
Chick Embryos ◽  
Embryonic Chick ◽  
White Leghorn ◽  
Lung Maturation ◽  
Synthetic Analogs ◽  
Lung Physiology ◽  
Avian Lung

Dexamethasone and other synthetic analogs of corticosteroids have been employed clinically as enhancers of lung development. The mechanism(s) by which this steroid induction of later lung maturation operates is not clear. This study reports the effect on lung epithelia of dexamethasone administered at different intervals during development. White Leghorn chick embryos were used so as to remove possible maternal and placental influences on the exogenously applied steroid. Avian lung architecture does vary from mammals; however, respiratory surfactant produced by the lung epithelia serves an equally critical role in avian lung physiology.

Semi-synthesis as a tool for broadening the health applications of bioactive olive secoiridoids: a critical review

2021 ◽  
Author(s):  
Manuela Oliverio ◽  
Monica Nardi ◽  
Maria Luisa Di Gioia ◽  
Paola Costanzo ◽  
Sonia Bonacci ◽  
...  
Keyword(s):  
Critical Review ◽  
Natural Compounds ◽  
Effective Strategy ◽  
Synthetic Analogues ◽  
Health Applications ◽  
Natural And Synthetic

Semi-synthesis is an effective strategy to obtain both natural and synthetic analogues of the olive secoiridoids, starting from easy accessible natural compounds.

Antitranspirant action of abscisic acid and ten synthetic analogs in black spruce

1990 ◽  
Vol 80 (3) ◽  
pp. 365-370 ◽  
Author(s):  
Terence J. Blake ◽  
Weixing Tan ◽  
Suzanne R. Abrams
Keyword(s):  
Abscisic Acid ◽  
Black Spruce ◽  
Synthetic Analogs
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