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Enzyme inhibitory
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The study on essential oils of various plantparts and their biological activities continues to be an important area of research and developmen. In the continuation of our current research on the identification of bioactive substances from plants of North East India.
21p
viamancio
04-06-2024
2
0
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The essential oils were also tested for their antioxidant, anti-imflammatory, antimicrobial and cytotoxic activities. The HD essential oil sample showed inhibitory activity against 6/8 tested microorganisms, i.e., Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, Bacillus subtillis, Candida albicans, and Saccharomyces cerevisiae. The MHD and EHD exhibited the inhibitory activity against three strains E. coli, A. niger and F. oxysporum. The UHD inhibited E. coli and F. oxysporum.
9p
dianmotminh02
03-05-2024
8
1
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The synthesized compounds' enzyme inhibition potential was tested against a-glucosidase, AChE, and BChE enzymes. As illustrated from the results of IC50, these compounds are observed as the active inhibitory potential for these enzymes. The cytotoxic activity by hemolytic Assay revealed that these compounds have mild exposure to cytotoxicity on RBCs.
10p
visergey
02-04-2024
0
0
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Using the natural agents with inhibitory activity against digestive enzymes α-glucosidase and αamylase capable of hydrolyzing carbohydrates into glucose to reduce blood glucose levels in the blood is one of the effective strategies to control diabetes, especially type II diabetes. α-Mangostin (AMG) was proven to have strong biological activities, such as antifungal, antibacterial, anti-inflammatory, anti-cancer.
9p
vimulcahy
18-09-2023
2
2
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Pancreatic lipase is one of the safest targets of anti-obesity drugs. To date, orlistat is the only pancreatic lipase inhibitor approved for the long-term treatment of obesity. Therefore, there is an elevated need to find new drugs for this disease. Determining the factors affecting the test to evaluate pancreatic lipase inhibitory activity in order to build a standard assay procedure is necessary. This will make it much easier for researchers to find novel compounds that inhibit the enzyme.
6p
viwolverine
07-07-2023
7
1
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In this research, we describe the isolation and structural elucidation of six compounds (1-6) from the aerial of C. asiaticum and their inhibitory activities on NO production and enzyme acetylcholinesterase.
9p
vineville
08-02-2023
1
1
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In this paper, we have prepared peripherally tetra-({6-[3-(diethylamino)phenoxy]hexyl}oxy substituted cobalt(II), copper(II), manganese(III) phthalocyanines (3, 4, 5) and their water-soluble derivatives (3a, 4a, 5a). Then, in vitro α-glucosidase and cholinesterases inhibitory actions of the water-soluble 3a, 4a, 5a were examined using spectrophotometric methods. 4a had the highest inhibitory effects among the tested compounds against α-glucosidase due to IC50 values. 4a and 5a had 40 fold higher inhibitory effects than the positive control.
11p
lyhuyenthu
31-01-2023
7
2
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In this study, we determined the in vitro inhibitory effects of metal ions such as Cu2+, Cd2+, Ag+, and Co2+ on GST enzyme activity. For this aim, GST was purified from C. tarichi Pallas liver with 37.36% yield and 29.304 EU/mg specific activity using the chromatographic method. The Vmax values of liver GST were determined for CDNB and GSH to be 1.245 and 0.562 EU/mL, respectively, and the Km values were found 0.89 and 0.06 mM, respectively, using the Lineweaver–Burk plot.
8p
lyhuyenthu
31-01-2023
3
2
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The aim of the present study was to synthesize and characterize benzothiazine derivatives prepared by using 2-aminothiophenol and saccharine and in vitro screen their enzyme inhibition and antioxidant potential. Nine different derivatives were prepared and their structures were confirmed by spectral studies (EIMS, 1H and 13 C NMR). Enzyme inhibition potential of the synthesized compounds was evaluated by Ellman’s method, while antioxidant activity was determined by DPPH and FRAP assays.
9p
langthannam
29-12-2021
12
0
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The compounds were identified by the use of 1D- and 2D-NMR and UV spectroscopic techniques and by comparisons with the reported data. The acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of the acetone, methanol, and water extracts of the plant and of the flavones penduletin and apigenin were evaluated at 200 µg/mL. The water extract exhibited better activity against the enzyme AChE as compared to both the acetone and the methanol extracts. Penduletin (1) showed significant activity against BChE (66.
9p
langthannam
29-12-2021
10
0
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The self-condensation reaction of benzoyl dialkyl phosphonates was developed using cyanide ion as catalyst, affording versatile tertiary O-protected α-hydroxy phosphonates in moderate yield. Hydroxy phosphonic acids and their ester derivatives have gained considerable attention due to their inhibitory activity towards various important groups of enzymes.
8p
langthannam
29-12-2021
9
0
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In addition, optimum ionic strength, optimum pH, optimum temperature, and stable pH values were determined for the enzyme in the kinetic studies performed. K M and Vmax were determined for NADPH and cytochrome c. Effects of some metals ions, antibiotics, and some other drugs used in aquarium fisheries on the activity of the enzyme were investigated. IC50 values and Ki values of metals showing an inhibitory effect were calculated.
10p
langthannam
29-12-2021
4
0
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Heterocyclic compounds with diaryl substituents have been a milestone approach for selective cyclooxygenase 2 (COX 2) inhibition by bioisosteric replacements and modifications. It is also known that thiazole derivatives have different pharmacological activities. In this study, nine novel 2-[(1,5-diphenyl-1H-imidazole-2-yl)thio]-N-(thiazole-2-yl)acetamide derivatives (Compound 1-9) were synthesized via the reaction of 1,5-disubstitued phenyl-imidazole-2-thiole and N-thiazole acetamide. The inhibitory effects of COX-1 and COX-2 enzymes were tested for the synthesized compounds
45p
langthannam
29-12-2021
12
0
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In silico studies reports that their physicochemical, ADMET and druglikeness properties were found to be in standard limit, which infers that, these compounds may not have problems with oral bioavailability. Molecular docking studies showed that the pyrimidines have better enzyme inhibitory activity onTMPKmt.
4p
mudbound
10-12-2021
7
1
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A series of new thiazole-hydrazones (3a–3n) were synthesized, characterized, and screened for their hMAOA and hMAO-B inhibitory activity by an in vitro fluorometric method. Selectivity indexes (SIs) were expressed as IC50 (MAO-A) / IC50 (MAO-B). Compound 3f showed promising hMAO-A inhibition with an IC50 value of 1.20 µM and displayed a very significant SI of 0.04 towards hMAO-A. The mechanism of hMAO-A inhibition was investigated by enzyme kinetics using Lineweaver–Burk graphics.
15p
tudichquannguyet
29-11-2021
8
0
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Twenty-five new hydroxy- and methoxy-substituted 4,6-diarylpyrimidin-2(1H)-ol (20–34) and 4,6-diarylpyrimidine-2(1H)-thiol derivatives (35–44) were synthesized from the reaction of the corresponding 1,3-diaryl-2-propene-1- one compounds (1–19) with urea or thiourea using the solid-phase microwave method. All the new synthetic compounds (20–44) were evaluated with regard to their α-glucosidase activity. However, only compounds 22–25, 27, 31, 34, 35, 37, and 40 exhibited a greater inhibitory effect than standard acarbose. The IC50 values of the active compounds ranged between 2.36 and 13.
16p
tudichquannguyet
29-11-2021
9
1
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The discovery of enzyme targeting inhibitors is a popular area of drug research. Biological activities of the compounds bearing phenol and heteroaryl groups make them popular groups in drug design targeting important enzymes such as acetylcholinesterase (AChE, E.C.3.1.1.7) and carbonic anhydrases (CAs, EC 4.2.1.1). The compounds 2 and 4 were found potent AChE inhibitors with the Ki values of 22.13 ±1.96 nM and 23.71 ±2.95 nM, respectively, while the compounds 2 (Ki = 8.61 ±0.90 nM, on hCA I) and 1 (Ki = 8.76 ±0.84 nM, on hCA II) had considerable CAs inhibitory potency.
10p
tudichquannguyet
29-11-2021
10
1
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The investigation of carbonic anhydrase and paraoxonase enzyme inhibition properties of water-soluble zinc and gallium phthalocyanine complexes (1 and 2) are reported for the first time. The binding of p-sulfonylphenoxy moieties to the phthalocyanine structure favors excellent solubilities in water, as well as providing an inhibition effect on carbonic anhydrase (CA) I and II isoenzymes and paraoxonase (PON1) enzyme. According to biological activity results, both complexes inhibited hCA I, hCA II, and PON1.
13p
tudichquannguyet
29-11-2021
15
1
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N-(1-(4-Methoxyphenyl)-3-oxo-3-((4-(N-(substituted)sulfamoyl)phenyl)amino)prop-1-en-1-yl)benzamides 3a – g were designed since sulfonamide and benzamide pharmacophores draw great attention in novel drug design due to their wide range of bioactivities including acetylcholinesterase (AChE) and human carbonic anhydrase I and II (hCA I and hCA II) inhibitory potencies. Structure elucidation of the compounds was carried out by 1 H NMR, 13C NMR, and HRMS spectra.
28p
tudichquannguyet
29-11-2021
13
1
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In this study, a new series of Mannich bases, 3-(aminomethyl)-6-{3-[4-(trifluoromethyl)phenyl]acryloyl}-2(3H)- benzoxazolones (1a–g), were synthesized by the Mannich reaction. Inhibitory effects of the newly synthesized compounds towards carbonic anhydrases (CAs) and acetylcholinesterase (AChE) enzymes were evaluated to find out new potential drug candidate compounds. According to the inhibitory activity results, Ki values of the compounds 1 and 1a–g were in the range of 12.3 ± 1.2 to 154.0 ± 9.3 nM against hCA I, and they were in the range of 8.6 ± 1.9 to 41.0 ± 5.5 nM against hCA II.
14p
tudichquannguyet
29-11-2021
6
1
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