Synthesis of novel tris-chalcones and determination of their inhibition profiles against some metabolic enzymes.
04 Mar 2021-Archives of Physiology and Biochemistry (Informa UK Limited)-Vol. 127, Iss: 2, pp 153-161
TL;DR: The results revealed that novel tris-chalcones can have promising drug potential for glaucoma, leukaemia, epilepsy; Alzheimer’s disease that was associated with the high enzymatic activity of hCA I, hCA II, AChE, and BChE enzymes.
Abstract: In this study, we report the synthesis of novel tris-chalcones and testing of human carbonic anhydrase I, and II isoenzymes (hCA I, and hCA II), acetylcholinesterase (AChE), butyrylcholinesterase (...
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TL;DR: In this article, a series of pyrrole-3-one derivatives containing sulfa drugs (5a-i) were determined to be highly potent inhibitors for AChE and human carbonic anhydrase (hCA) isoenzymes.
Abstract: Human carbonic anhydrase (hCA) isoenzymes are zinc ion-containing, widespread metalloenzymes and they classically play a role in pH homeostasis maintenance. CA inhibitors suppress the CA activity and their usage has been clinically established as antiglaucoma agents, antiepileptics, diuretics, and in some other disorders. Alzheimer's disease (AD) is a slowly progressive neurodegenerative disorder and a fatal disease of the brain. An advanced method to cure AD includes the strategy to design acetylcholinesterase (AChE) inhibitors. A novel series of pyrrole-3-one derivatives containing sulfa drugs (5a-i) were determined to be highly potent inhibitors for AChE and hCA I and hCA II (inhibitory constant [Ki ] values are in the range of 6.50 ± 1.02-37.46 ± 4.12 nM, 1.20 ± 0.19-44.21 ± 1.09 nM, and 8.93 ± 1.58-46.86 ± 8.41 nM for AChE, hCA I, and hCA II, respectively). The designed compounds often show a more effective inhibition than the chemicals used as the standard. Among these compounds, 5f was the most effective compound against hCA I, and compound 5e was the most effective compound against hCA II. It was determined that compound 5c was the most effective inhibitor for AChE.
100 citations
01 Jan 2014
TL;DR: Sulphamides and sulphonamides are important biologically active compounds as mentioned in this paper and have potential use in the treatment of depression,neuropathic and inflammatory pains.
Abstract: Sulphamides [1] and sulphonamides [2] are importantbiologically active compounds. In the last decades a lot ofsulphamide and sulphonamide drugs have appeared inthe markets. Quinagolide (1), a dopaminergic drug, isan antihyperprolactinemia agent [3]. Compound 2 (JNJ-26990990) has potential use in the treatment of depression,neuropathic and inflammatory pains [4]. The sulphonamidedrug sultiame (3) is an anticonvulsant used in the treatmentof epilepsy and West syndrome [5]. Acetazolamide (AZA, 4), adrug alsoknownas carbonicanhydrase (CA) inhibitor,isusedin the treatment of glaucoma [6] and idiopathic intracranialhypertension [7] (Figure 1).CA (E.C.: 4.2.1.1) is a protein that is well suited to serve as amodel in many types of biophysical, bioanalytical andphysical-organic chemical studies as well as for inhibitordrug design studies. This enzyme catalyses the hydration ofcarbon dioxide (CO
91 citations
TL;DR: Ethanolic (EEC) and aqueous (WEC) extracts of cinnamon (Cinnamomum verum) were evaluated for their antioxidant profiles by eight distinguished bioanalytical antioxidant methods.
Abstract: Ethanolic (EEC) and aqueous (WEC) extracts of cinnamon (Cinnamomum verum) were evaluated for their antioxidant profiles by eight distinguished bioanalytical antioxidant methods. Their inhibitory ef...
78 citations
Cites background from "Synthesis of novel tris-chalcones a..."
...For the reduction of body weight and control of the blood glucose level, specific inhibitors can inhibit the both digestive enzymes.([105]) The WEC and EEC exhibited IC50 values of 189....
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TL;DR: Nimodipine presented the highest docking score and had competitive inhibition, the benzene and pyridine rings were found to enter the cavity for hCA I, and these compounds may be useful for CA inhibitors.
Abstract: Carbonic anhydrases (CAs) are potent dehydration of carbonic acid and catalyst of the reversible hydration of carbon dioxide. Here, CA I and CA II was purified from human erythrocytes using the sim...
56 citations
TL;DR: The docking studies showed that compound 5b could be inserted into the active pocket of α-glucosidase and form hydrogen bonds with LYS293 to enhance the binding affinity and prove that their inhibition was reversible and a mixed type.
53 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 of novel tris-chalcones a..." refers methods in this paper
...SDS-PAGE was used for screening of hCA isoenzymes (Laemmli 1970) as described in previous studies (Çoban et al....
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...SDS-PAGE was used for screening of hCA isoenzymes (Laemmli 1970) as described in previous studies (Çoban et al. 2008)....
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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 of novel tris-chalcones a..." refers methods in this paper
...Bradford (1976) method was used for the determination of the quantity of protein during the purification steps as described in detail (Çoban et al. 2007)....
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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 of novel tris-chalcones a..." refers methods in this paper
...The inhibitory effect of novel tris-chalcones (23–34) on AChE/BChE activities was performed according to Ellman’s method (Ellman et al. 1961) as described previously (Maharramov et al. 2019)....
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...The inhibition properties of novel tris-chalcones (23–34) against AChE and BChE were performed according to Ellman’s procedure (Ellman et al. 1961) as described in detail in a previous study (Tao et al. 2013)....
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TL;DR: On the basis of the assumed theory the rate of the observed reaction is directly proportional to the concentration of the enzyme-substrate compound, where (E:l = (ES).
Abstract: On the basis of the assumed theory the rate of the observed reaction is directly proportional to the concentration of the enzyme-substrate compound, (ES), a t all values of the concentration of the substrate, (S). It is proportional to (S) only a t low values of (S). The numerical value of the dissociation constant is given by the substrate concentration a t half-maximum velocity, where (E:l = (ES). The equilibrium in equation 1 may be heterogeneous or homogeneous. Hitchcock'\" has pointed
11,349 citations
Additional excerpts
...Then, the Lineweaver–Burk graphs were drawn (Lineweaver and Burk 1934)....
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