Phenserine, a Novel Anticholinesterase Related to Physostigmine: Total Synthesis and Biological Properties

1996 ◽  
Vol 49 (2) ◽  
pp. 171 ◽  
Author(s):  
A Brossi ◽  
XF Pei ◽  
NH Greig
Keyword(s):  
Amyloid Precursor Protein ◽  
Total Synthesis ◽  
Active Form ◽  
Biological Properties ◽  
Optically Active ◽  
National Institutes Of Health ◽  
Drug Candidate ◽  
Experimental Animals ◽  
Β Amyloid ◽  
Potential Use

Phenserine, the phenylcarbamate analogue of physostigmine , is a drug candidate of potential use for treating Alzheimer's disease. Phenserine inhibits acetylcholinesterase selectively, improves memory dramatically in experimental animals without toxicity, and reduces the production of β-amyloid precursor protein, the source of the Alzheimer's toxin β-amyloid. Phenserine was made from physostigmine in two steps, and it can be prepared in the required optically active form by total synthesis. For this purpose, the oxindole route developed by Julian in his total synthesis of physostigmine was vastly improved. Details of this work performed at the National Institutes of Health and at Institutions sponsored by this agency are presented herein.

Isolation, structure, and synthesis of chenopodanol and the absolute configuration of chenopodene and chenopodanol

1997 ◽  
Vol 75 (6) ◽  
pp. 634-640 ◽  
Author(s):  
Motoo Tori ◽  
Tomonobu Hamaguchi ◽  
Mamiko Aoki ◽  
Masakazu Sono ◽  
Yoshinori Asakawa
Keyword(s):  
Total Synthesis ◽  
Absolute Configuration ◽  
Active Form ◽  
Optically Active ◽  
Spectroscopic Techniques ◽  
The Absolute

(−)-Chenopodanol (2) has been isolated from the liverwort Marchantiachenopoda and its structure determined by spectroscopic techniques as well as by total synthesis. Chenopodene (1) has also been synthesized in an optically active form, resulting in revision of the originally assigned absolute configuration. Keywords: chenopodanol, chenopodene, liverwort, Marchantiachenopoda, sesquiterpene.

Total synthesis of zizaane sesquiterpenes: (−)-khusimone, (+)-zizanoic acid, and (−)-epizizanoic acid

1982 ◽  
Vol 60 (9) ◽  
pp. 1081-1091 ◽  
Author(s):  
Hsing-Jang Liu ◽  
Wing Hong Chan
Keyword(s):  
Total Synthesis ◽  
Ammonium Salt ◽  
Active Form ◽  
Optically Active ◽  
Camphorsulfonic Acid

Three sesquiterpenes of the zizaane family, khusimone (1), epizizanoic acid (3), and zizanoic acid (2) have been synthesized in optically active form from the ammonium salt of (−)-l-10-camphorsulfonic acid in sixteen, nineteen, and twenty steps respectively.

scholarly journals The β-Amyloid Precursor Protein APP Is Tyrosine-phosphorylated in Cells Expressing a Constitutively Active Form of the Abl Protoncogene

2001 ◽  
Vol 276 (23) ◽  
pp. 19787-19792 ◽  
Author(s):  
Nicola Zambrano ◽  
Paola Bruni ◽  
Giuseppina Minopoli ◽  
Rosario Mosca ◽  
Diana Molino ◽  
...  
Keyword(s):  
Amyloid Precursor Protein ◽  
Active Form ◽  
Precursor Protein ◽  
Β Amyloid ◽  
In Cells ◽  
Constitutively Active

The total synthesis of optically active annotinine

1969 ◽  
Vol 47 (3) ◽  
pp. 433-444 ◽  
Author(s):  
K. Wiesner ◽  
Lizzie Poon ◽  
I. Jirkovský ◽  
M. Fishman
Keyword(s):  
Total Synthesis ◽  
Active Form ◽  
Optically Active ◽  
Lycopodium Alkaloid

The total synthesis of the first Lycopodium alkaloid annotinine in the optically active form is described. The key step in this synthesis was the photochemical addition of allene to the tricyclic vinylogous imide (3) which yielded the photoadduct (6).

Tamarix articulata (T. articulata) - An Important Halophytic Medicinal Plant with Potential Pharmacological Properties

2019 ◽  
Vol 20 (4) ◽  
pp. 285-292 ◽  
Author(s):  
Abdullah M. Alnuqaydan ◽  
Bilal Rah
Keyword(s):  
Medicinal Plant ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
In Vivo Model ◽  
Drug Candidate ◽  
Phytochemical Analysis ◽  
Pharmacological Properties

Background:Tamarix Articulata (T. articulata), commonly known as Tamarisk or Athal in Arabic region, belongs to the Tamaricaece species. It is an important halophytic medicinal plant and a good source of polyphenolic phytochemical(s). In traditional medicines, T. articulata extract is commonly used, either singly or in combination with other plant extracts against different ailments since ancient times.Methods:Electronic database survey via Pubmed, Google Scholar, Researchgate, Scopus and Science Direct were used to review the scientific inputs until October 2018, by searching appropriate keywords. Literature related to pharmacological activities of T. articulata, Tamarix species, phytochemical analysis of T. articulata, biological activities of T. articulata extracts. All of these terms were used to search the scientific literature associated with T. articulata; the dosage of extract, route of administration, extract type, and in-vitro and in-vivo model.Results:Numerous reports revealed that T. articulata contains a wide spectrum of phytochemical(s), which enables it to have a wide window of biological properties. Owing to the presence of high content of phytochemical compounds like polyphenolics and flavonoids, T. articulata is a potential source of antioxidant, anti-inflammatory and antiproliferative properties. In view of these pharmacological properties, T. articulata could be a potential drug candidate to treat various clinical conditions including cancer in the near future.Conclusion:In this review, the spectrum of phytochemical(s) has been summarized for their pharmacological properties and the mechanisms of action, and the possible potential therapeutic applications of this plant against various diseases discussed.

Plant Extracts and their Secondary Metabolites as Modulators of Kinases

2020 ◽  
Vol 20 (12) ◽  
pp. 1093-1104 ◽  
Author(s):  
Muhammad Shoaib Ali Gill ◽  
Hammad Saleem ◽  
Nafees Ahemad
Keyword(s):  
Signal Transduction ◽  
Secondary Metabolites ◽  
Plant Extracts ◽  
Cell Biology ◽  
Kinase Inhibitor ◽  
Plant Secondary Metabolites ◽  
Biological Properties ◽  
Drug Candidate ◽  
New Chemical Entities ◽  
Natural Flora

Natural Products (NP), specifically from medicinal plants or herbs, have been extensively utilized to analyze the fundamental mechanisms of ultimate natural sciences as well as therapeutics. Isolation of secondary metabolites from these sources and their respective biological properties, along with their lower toxicities and cost-effectiveness, make them a significant research focus for drug discovery. In recent times, there has been a considerable focus on isolating new chemical entities from natural flora to meet the immense demand for kinase modulators, and also to overcome major unmet medical challenges in relation to signal transduction pathways. The signal transduction systems are amongst the foremost pathways involved in the maintenance of life and protein kinases play an imperative part in these signaling pathways. It is important to find a kinase inhibitor, as it can be used not only to study cell biology but can also be used as a drug candidate for cancer and metabolic disorders. A number of plant extracts and their isolated secondary metabolites such as flavonoids, phenolics, terpenoids, and alkaloids have exhibited activities against various kinases. In the current review, we have presented a brief overview of some important classes of plant secondary metabolites as kinase modulators. Moreover, a number of phytocompounds with kinase inhibition potential, isolated from different plant species, are also discussed.

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