Synthesis and biological evaluation of novel tris-chalcones as potent carbonic anhydrase, acetylcholinesterase, butyrylcholinesterase and α-glycosidase inhibitors.
TL;DR: These derivatives' inhibitory potential on the tested enzymes are promising drug candidates for the treatment of diseases like glaucoma, leukemia, epilepsy; Alzheimer's disease; type-2 diabetes mellitus that are associated with high enzymatic activity of carbonic anhydrase, acetylcholine esterase, butyrylcholinesterases, and α-glycosidase.
About: This article is published in Bioorganic Chemistry.The article was published on 2019-01-02. It has received 137 citations till now. The article focuses on the topics: Carbonic Anhydrase I & Butyrylcholinesterase.
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TL;DR: A series of substituted pyrazole compounds were synthesized and their structure was characterized by IR, NMR, and Mass analysis and emerged as effective inhibitors of the cytosolic carbonic anhydrase I and II isoforms and acetylcholinesterase enzymes with Ki values in the range of 1.23-22.65 ± 5.36 µM.
143 citations
TL;DR: The synthesis, crystal structure, characterization, and enzyme inhibition effects of the novel a series of 2-aminopyridine liganded Pd(II) N-heterocyclic carbene (NHC) complexes were examined and the inhibition effect of these derivatives on aldose reductase and α-glycosidase enzymes was studied.
125 citations
TL;DR: The novel synthesized compounds (MZ1-MZ11) have a higher enzyme inhibitory potential than ACR, TAC, and AZA, respectively and may have the potential to be used as alternative medicines after further research in the treatment of many diseases such as diabetes, Alzheimer's disease, heart failure, ulcer, and epilepsy.
103 citations
TL;DR: ADME prediction study of the designed N-substituted phthalazine sulfonamides showed that they are not only with carbonic anhydrase and acetylcholinesterase inhibitory activities but also with appropriate pharmacokinetic, physicochemical parameters and drug-likeness properties.
99 citations
References
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TL;DR: Using an improved method of gel electrophoresis, many hitherto unknown proteins have been found in bacteriophage T4 and some of these have been identified with specific gene products.
Abstract: Using an improved method of gel electrophoresis, many hitherto unknown proteins have been found in bacteriophage T4 and some of these have been identified with specific gene products. Four major components of the head are cleaved during the process of assembly, apparently after the precursor proteins have assembled into some large intermediate structure.
232,912 citations
"Synthesis and biological evaluation..." refers methods in this paper
...Sodium dodecyl sulphate-polyacrylamide gel electrophoresis (SDSPAGE) was used for fixation of both isoenzymes [72] described in previous studies [73]....
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TL;DR: This assay is very reproducible and rapid with the dye binding process virtually complete in approximately 2 min with good color stability for 1 hr with little or no interference from cations such as sodium or potassium nor from carbohydrates such as sucrose.
225,085 citations
"Synthesis and biological evaluation..." refers methods in this paper
...change at 348 nm of PNA to 4-nitrophenylate over a period of 3min at 25 °C [71]....
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...Bradford technique was used for the investigation of protein amount during the purification stages [71]....
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Journal Article•
TL;DR: Using an improved method of gel electrophoresis, many hitherto unknown proteins have been found in bacteriophage T4 and some of these have been identified with specific gene products as mentioned in this paper.
Abstract: Using an improved method of gel electrophoresis, many hitherto unknown proteins have been found in bacteriophage T4 and some of these have been identified with specific gene products. Four major components of the head are cleaved during the process of assembly, apparently after the precursor proteins have assembled into some large intermediate structure.
203,017 citations
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.
23,015 citations
"Synthesis and biological evaluation..." refers methods in this paper
...rivatives (5a-5i) on AChE/BChE activities was performed according to Ellman’s method [60] as described previously [76]....
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16,894 citations
"Synthesis and biological evaluation..." refers background in this paper
...CeF bond make it important to be examined in the class of drug candidate compounds containing fluorine [5]....
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