Journal ArticleDOI
Coumarins as cholinesterase inhibitors: A review.
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TLDR
The studies and development of new compounds for AD treatment are discussed, which objective is to increase the concentration of ACh in the synaptic cleft by the inhibition of cholinesterases.About:
This article is published in Chemico-Biological Interactions.The article was published on 2016-07-25. It has received 111 citations till now. The article focuses on the topics: Synaptic cleft.read more
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Coumarin: A Natural, Privileged and Versatile Scaffold for Bioactive Compounds
TL;DR: An overview of the most recent synthetic pathways leading to mono- and polyfunctionalized coumarins will be presented, along with the main biological pathways of their biosynthesis and metabolic transformations.
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Plant extracts for developing mosquito larvicides: From laboratory to the field, with insights on the modes of action.
TL;DR: This review covers the huge amount of literature available on plant extracts tested as mosquito larvicides, particularly aqueous and alcoholic ones, due to their easy formulation in water without using surfactants, and concludes that 29 of them have outstanding larvicidal activity against major vectors belonging to the genera Anopheles, Aedes and Culex.
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Copper nanoparticles as inexpensive and efficient catalyst: A valuable contribution in organic synthesis
Nisha Kant Ojha,Grigory V. Zyryanov,Grigory V. Zyryanov,Adinath Majee,Valery N. Charushin,Valery N. Charushin,Oleg N. Chupakhin,Oleg N. Chupakhin,Sougata Santra +8 more
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An overview of coumarin as a versatile and readily accessible scaffold with broad-ranging biological activities
TL;DR: This review is intended to be a critical overview on coumarins, comprehensive of natural sources, metabolites, biological evaluations and synthetic approaches.
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Novel tacrine-coumarin hybrids linked to 1,2,3-triazole as anti-Alzheimer’s compounds: In vitro and in vivo biological evaluation and docking study
Zahra Najafi,Mohammad Mahdavi,Mina Saeedi,Elahe Karimpour-Razkenari,Najmeh Edraki,Mohammad Sharifzadeh,Mahnaz Khanavi,Tahmineh Akbarzadeh +7 more
TL;DR: In vivo studies by Morris water maze task showed that compound 8e significantly reversed scopolamine-induced memory deficit in rats, and compound 8m displayed the best anti-BChE activity much more active than tacrine and donepezil as the reference drugs.
References
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Journal ArticleDOI
A new and rapid colorimetric determination of acetylcholinesterase activity.
TL;DR: A photometric method for determining acetylcholinesterase activity of tissue extracts, homogenates, cell suspensions, etc., has been described and Kinetic constants determined by this system for erythrocyte eholinesterases are presented.
Journal Article
Evaluation of a tetrazolium-based semiautomated colorimetric assay: assessment of chemosensitivity testing.
TL;DR: The clonogenic assay was more sensitive when continuous drug exposures were utilized, although this was primarily related to the increased drug exposure time, and therefore it offers a valid, simple method of assessing chemosensitivity in established cell lines.
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Drug-like properties and the causes of poor solubility and poor permeability
TL;DR: There are currently about 10000 drug-like compounds, and true diversity does not exist in experimental combinatorial chemistry screening libraries because current ADME experimental screens are multi-mechanisms, and predictions get worse as more data accumulates.
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Natural Products as Sources of New Drugs over the Period 1981−2002
TL;DR: From the data presented, the utility of natural products as sources of novel structures, but not necessarily the final drug entity, is still alive and well, and in the area of cancer, the percentage of small molecule, new chemical entities that are nonsynthetic has remained at 62% averaged over the whole time frame.
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Atomic structure of acetylcholinesterase from Torpedo californica: a prototypic acetylcholine-binding protein
Joel L. Sussman,Michal Harel,Felix Frolow,Christian Oefner,Adrian Goldman,Lilly Toker,Israel Silman +6 more
TL;DR: Modeling of acetylcholine binding to the enzyme suggests that the quaternary ammonium ion is bound not to a negatively charged "anionic" site, but rather to some of the 14 aromatic residues that line the gorge.