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Synthesis and discovery of potent carbonic anhydrase, acetylcholinesterase, butyrylcholinesterase, and alpha-glycosidase enzymes inhibitors: The novel N,N '-bis-cyanomethylamine and alkoxymethylamine derivatives
(Wiley, 2018-04)
During this investigation, N,N'-bis-azidomethylamines, N,N'-bis-cyanomethylamine, new alkoxymethylamine and chiral derivatives, which are considered to be a new generation of multifunctional compounds, were synthesized, ...
Synthesis of 4,5-disubstituted-2-thioxo-1,2,3,4-tetrahydropyrimidines and investigation of their acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase I/II inhibitory and antioxidant activities
(Informa, 2016-12)
A series of tetrahydropyrimidinethiones were synthesized from thiourea, -diketones and aromatic aldehydes, such as p-tolualdehyde, p-anisaldehyde, o-tolualdehyde, salicylaldehyde and benzaldehyde. These cyclic thioureas ...
The first synthesis of 4-phenylbutenone derivative bromophenols including natural products and their inhibition profiles for carbonic anhydrase, acetylcholinesterase and butyrylcholinesterase enzymes
(Elsevier, 2017-06)
The first synthesis of (E)-4-(3-bromo-4,5-dihydroxyphenyl) but-3-en-2-one (1), (E)-4-(2-bromo-4,5-dihy droxyphenyl) but-3-en-2-one (2), and (E)-4-(2,3-dibromo-4,5-dihydroxyphenyl) but-3-en-2-one (3) was realized as natural ...
Synthesis, characterization, and SAR of arylated indenoquinoline‐based cholinesterase and carbonic anhydrase inhibitors
(Wiley, 2018-09)
We report the synthesis of bromoindenoquinolines (15a-f) by Friedlander reactions in low yields (13-50%) and the conversion of the corresponding phenyl-substituted indenoquinoline derivatives 16-21 in high yields (80-96%) ...
Antioxidant activity, acetylcholinesterase, and carbonic anhydrase inhibitory properties of novel ureas derived from phenethylamines
(Wiley, 2016-12)
A series of ureas derived from phenethylamines were synthesized and evaluated for human carbonic anhydrase (hCA) I and II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzyme inhibitory activities and ...
Novel sulfamate derivatives of menthol: Synthesis, characterization, and cholinesterases and carbonic anhydrase enzymes inhibition properties
(Wiley, 2018-11)
Sulfamates have a large spectrum of biological activities including enzyme inhibition. Eight sulfamates derived from menthol (2a-h) were synthesized. Also, in the other section of this study, novel sulfamate derivatives ...
Meta-Cyanobenzyl substituted benzimidazolium salts: Synthesis, characterization, crystal structure and carbonic anhydrase, -glycosidase, butyrylcholinesterase, and acetylcholinesterase inhibitory properties
(Wiley, 2018-07)
meta-Cyanobenzyl-substituted N-heterocyclic carbene (NHC) precursors were synthesized by the reaction of a series of N-(alkyl)benzimidazolium with 3-bromomethyl-benzonitrile. These benzimidazolium salts were characterized ...
Some pyrazoles derivatives: Potent carbonic anhydrase, α‐glycosidase, and cholinesterase enzymes inhibitors
(Wiley, 2018-10)
A series of substituteed pyrazol-4-yl-diazene derivatives were found to be effective inhibitors against -glycosidase, cytosolic carbonic anhydrase I and II isoforms (hCA I and II), butyrylcholinesterase (BChE), and ...
Multiple studies have been recorded on the synthesis and design of multi‐aim anti‐Alzheimer molecules. Using dual butyrylcholinesterase/acetylcholinesterase inhibitor molecules has attracted more interest in the therapy for Alzheimer’s disease. In this study, a tannic acid compound showed excellent inhibitory effects against acetylcholine esterase (AChE), α‐glycosidase, α‐amylase, and butyrylcholinesterase (BChE). IC50 values of tannic acid obtained 11.9 nM against α‐glycosidase and 3.3 nM against α‐amylase, respectively. In contrast, Ki values were found of 50.96 ± 2.18 μM against AChE and 53.17 ± 4.47 μM against BChE. α‐Glycosidase inhibitor compounds can be utilized as a novel group of antidiabetic drugs. By competitively decreasing glycosidase activity, these inhibitor molecules help to hamper the fast breakdown of sugar molecules and thereby control the blood sugar level.
(Bentham Science, 2019)
Background: The present paper focuses on the in vitro inhibition of some sedative drugs such as Midazolam, Propofol, Hipnodex, Ketamine, and Pental sodium on acetylcholinesterase (AChE), Butyrylcholinesterase (BChE), and ...
Discovery of potent carbonic anhydrase, acetylcholinesterase, and butyrylcholinesterase enzymes inhibitors: The new amides and thiazolidine-4-ones synthesized on an acetophenone base
(Wiley, 2017-09)
Compounds containing nitrogen and sulfur atoms can be widely used in various fields, including industry, medicine, biotechnology, and chemical technology. Among them, amides of acids and heterocyclic compounds have an ...