Synthesis and Characterization of Triazole-Linked Bistetrahydrobenzofuran Derivatives as Anti-Ulcer Agents

2014 ◽  
Vol 997 ◽  
pp. 128-131
Author(s):  
Quan Li Yang ◽  
Chun Xue Chen ◽  
Wu Li ◽  
Wan Liu ◽  
Hu Biao Fang ◽  
...  
Keyword(s):  
Elemental Analysis ◽  
Click Reaction ◽  
Bioactive Compound ◽  
Inhibitory Effect ◽  
Synthesis And Characterization ◽  
Mild Conditions ◽  
Inhibitory Activities ◽  
High Yields

A pair of triazole-linked bistetrahydrobenzofuran derivatives were prepared in high yields through Cu (II)-catalyzed click reaction under mild conditions. All of the intermediates and target compounds were characterized by NMR, IR, ESI-MS and elemental analysis. Thein vitroH+/K+-ATPase inhibitory effect for the target compounds were also evaluated by MTT methods, and the (E)-isomer of the bistetrahydrobenzofurans exhibited the better H+/K+-ATPase inhibitory activities than the commercial omeprazole with the IC50of 37.90 μM. The bioactive compound might be potentially used as anti-ulcer agents in the treatment of acid-related diseases.

Synthesis and In Vitro Anti-Ulcer Effect of Triazolo-Methyl Tetrahydrobenzofuran Oxime Ether Derivatives

2013 ◽  
Vol 746 ◽  
pp. 35-39 ◽  
Author(s):  
Hu Biao Fang ◽  
Lei Jin ◽  
Cheng Qiao Cao ◽  
Hua Jun Luo ◽  
Nian Yu Huang
Keyword(s):  
Elemental Analysis ◽  
Cycloaddition Reaction ◽  
Inhibitory Effect ◽  
Dipolar Cycloaddition ◽  
Reaction Sequence ◽  
Oxime Ether ◽  
Esi Ms ◽  
Mild Conditions ◽  
Activity Evaluation

The triazolo-methyl tetrahydrobenzofuran oxime ether isomers were prepared through Cu (II)-catalyzed Huisgen 1,3-dipolar cycloaddition reaction in a high-yielding three-step reaction sequence under mild conditions. All of the intermediates and target compounds were characterized by NMR, IR, ESI-MS and elemental analysis. Thein vitroanti-ulcer activity evaluation indicated the (Z)-oxime isomer of triazolo-methyl tetrahydrobenzofuran oxime ether exhibited most potent H+/K+-ATPase inhibitory effect with the IC50˰̵̱̼͆ͅ˰̶̿˰̅˾́̅˰μ̝˾ These compounds could be potentially used as anti-ulcer agents for the treatment of acid related diseases.

Synthesis and characterization of alkyl- and acyl-substituted oxime–phosphazenes

2005 ◽  
Vol 83 (12) ◽  
pp. 2039-2045 ◽  
Author(s):  
Erol Çil ◽  
Mustafa Arslan ◽  
Ahmet Orhan Görgülü
Keyword(s):  
Nmr Spectroscopy ◽  
Key Words ◽  
Elemental Analysis ◽  
Allyl Bromide ◽  
Ethyl Bromide ◽  
Synthesis And Characterization ◽  
Oxime Derivatives ◽  
High Yields

Two oxime–cyclophosphazenes were prepared from the hexakis(4-formylphenoxy)cyclotriphosphazene (2) and hexakis(4-acetylphenoxy)cyclotriphosphazene (8). The reactions of these oximes with ethyl bromide, allyl bromide, propanoyl chloride, and acriloyl chloride were studied. Hexasubstituted compounds were obtained from the reactions of hexakis{4-[(hydroxyimino)methyl]phenoxy}cyclotriphosphazene (3) with ethyl bromide (4), allyl bromide (5), and propanoyl chloride (6), however, the oxime groups on 3 rearranged to nitrile (7) in the reaction of 3 with acriloyl chloride. Hexasubstituted compounds were also obtained from the reactions of hexakis{4-[(1)-N-hydroxyethaneimidoyl]phenoxy}cyclotriphosphazene (9) with allyl bromide (11) and propanoyl chloride (12). Tetra- and penta-substituted products were obtained from the reactions of 9 with ethyl bromide (10) and acriloyl chloride (13), respectively. All products were generally obtained in high yields. The structures of the compounds were defined by elemental analysis, IR, 1H, 13C, and 31P NMR spectroscopy. Key words: hexachlorocyclotriphosphazene, phosphazene, oxime, oxime derivatives, oxime–phosphazenes.

Synthesis and characterization of new inhibitors of cholinesterases based on N-phenylcarbamates: In vitro study of inhibitory effect, type of inhibition, lipophilicity and molecular docking

2018 ◽  
Vol 78 ◽  
pp. 280-289 ◽  
Author(s):  
Katarína Vorčáková ◽  
Magdaléna Májeková ◽  
Eva Horáková ◽  
Pavel Drabina ◽  
Miloš Sedlák ◽  
...  
Keyword(s):  
Molecular Docking ◽  
In Vitro Study ◽  
Inhibitory Effect ◽  
Vitro Study ◽  
Synthesis And Characterization

scholarly journals α-Amylase and α-glucosidase inhibitory activities of the extracts and constituents of Ferulago blancheana, F. pachyloba and F. trachycarpa roots

2018 ◽  
Vol 13 (1) ◽  
pp. 35 ◽  
Author(s):  
Songül Karakaya ◽  
Hilal Özbek ◽  
Sefa Gözcü ◽  
Zühal Güvenalp ◽  
Hafize Yuca ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Video Clip ◽  
Inhibitory Effect ◽  
In Vitro Bioassay ◽  
Bioassay Guided Fractionation ◽  
Full Screen ◽  
Inhibitory Activities ◽  
Sterol Mixture

<p>Eleven coumarins named osthole (1), imperatorin (2), bergapten (3), prantschimgin (4), grandivitinol (5), suberosin (6), xanthotoxin (7), felamidin (8), marmesin (9), umbelliferone (10), ulopterol (11), and a sterol mixture consisted of stigmasterol (12), β-sitosterol (13) were isolated from the roots of Ferulago blancheana, F. pachyloba and F. trachycarpa through in vitro bioassay-guided fractionation processes. The extracts and bioactive compounds were evaluated for their α-amylase and α-glucosidase activities. Among the tested compounds, felamidin and suberosin showed significant α-glucosidase inhibitory activity with IC<sub>50</sub> values of 0.4 and 0.9 mg/mL, respectively, when compared to the reference standard acarbose (IC<sub>50</sub> = 4.9 mg/mL). Grandivitinol (IC<sub>50</sub> = 20.0 mg/mL) had the lowest inhibitory effect. On the other hand, none of the tested extracts were found to be active on α-amylase inhibition. This is the first report on isolation, characterization of the bioactive compounds and evaluation the α-amylase and α-glucosidase inhibitory activities of these species.</p><p><strong>Video Clip of Methodology</strong>:</p><p>8 min 26 sec:   <a href="https://www.youtube.com/v/x0gakPjgXmc">Full Screen</a>   <a href="https://www.youtube.com/watch?v=x0gakPjgXmc">Alternate</a></p><p> </p>

scholarly journals Synthesis and Characterization of trans-Dichlorotetrakis(imidazole)cobalt(III) Chloride: A New Cobalt(III) Coordination Complex with Potential Prodrug Properties

2018 ◽  
Vol 2018 ◽  
pp. 1-7
Author(s):  
Kaila F. Hart ◽  
Natalie S. Joe ◽  
Rebecca M. Miller ◽  
Hannah P. Nash ◽  
David J. Blake ◽  
...  
Keyword(s):  
Ascorbic Acid ◽  
Cell Line ◽  
Elemental Analysis ◽  
Ligand Exchange ◽  
Low Cost ◽  
Cost Effective ◽  
Good Alternative ◽  
Synthesis And Characterization ◽  
High Yields

Numerous therapies for the treatment of cancer have been explored with increasing evidence that the use of metal-containing compounds could prove advantageous as anticancer therapeutics. Previous works on Ru(III) complexes suggest that structurally similar Co(III) complexes may provide good alternative, low-cost, effective prodrugs. Herein, a new complex, trans-[Co(imidazole)4Cl2]Cl (2), has been synthesized in high yields utilizing ligand exchange under refluxing conditions. The structure of 2 has been characterized by elemental analysis, 1H and 13C·NMR, ESI-MS, CV, and UV-Vis. The ability of 2 to become reduced in the presence of ascorbic acid was probed demonstrating the likely reduction of the Co(III) metal center to Co(II). In addition, preliminary cell line testing on 2 shows a lack of cytotoxicity.

scholarly journals Design, synthesis, molecular docking, and in vitro α-glucosidase inhibitory activities of novel 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines against yeast and rat α-glucosidase

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Fariba Peytam ◽  
Ghazaleh Takalloobanafshi ◽  
Toktam Saadattalab ◽  
Maryam Norouzbahari ◽  
Zahra Emamgholipour ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Docking Study ◽  
Rat Small Intestine ◽  
Molecular Docking Study ◽  
Design Synthesis ◽  
Mild Conditions ◽  
Glucosidase Inhibitors ◽  
Inhibitory Activities

AbstractIn an attempt to find novel, potent α-glucosidase inhibitors, a library of poly-substituted 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines 3a–ag have been synthesized through heating a mixture of 2-aminobenzimidazoles 1 and α-azidochalcone 2 under the mild conditions. This efficient, facile protocol has been resulted into the desirable compounds with a wide substrate scope in good to excellent yields. Afterwards, their inhibitory activities against yeast α-glucosidase enzyme were investigated. Showing IC50 values ranging from 16.4 ± 0.36 µM to 297.0 ± 1.2 µM confirmed their excellent potency to inhibit α-glucosidase which encouraged us to perform further studies on α-glucosidase enzymes obtained from rat as a mammal source. Among various synthesized 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines, compound 3k exhibited the highest potency against both Saccharomyces cerevisiae α-glucosidase (IC50 = 16.4 ± 0.36 μM) and rat small intestine α-glucosidase (IC50 = 45.0 ± 8.2 μM). Moreover, the role of amine moiety on the observed activity was studied through substituting with chlorine and hydrogen resulted into a considerable deterioration on the inhibitory activity. Kinetic study and molecular docking study have confirmed the in-vitro results.

scholarly journals In Vitro α-Glucosidase and α-Amylase Inhibitory Activities of Free and Bound Phenolic Extracts from the Bran and Kernel Fractions of Five Sorghum Grain Genotypes

Foods ◽  
2020 ◽  
Vol 9 (9) ◽  
pp. 1301
Author(s):  
Yun Xiong ◽  
Ken Ng ◽  
Pangzhen Zhang ◽  
Robyn Dorothy Warner ◽  
Shuibao Shen ◽  
...  
Keyword(s):  
Digestive System ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Inhibitory Effects ◽  
Phenolic Contents ◽  
Inhibitory Activities ◽  
Sorghum Grain ◽  
Global Health Challenge ◽  
Phenolic Extracts

Diabetes is a global health challenge. Currently, an effective treatment for diabetes is to reduce the postprandial hyperglycaemia by inhibiting the carbohydrate hydrolysing enzymes in the digestive system. In this study, we investigated the in vitro α-glucosidase and α-amylase inhibitory effects of free and bound phenolic extracts, from the bran and kernel fractions of five sorghum grain genotypes. The results showed that the inhibitory effect of sorghum phenolic extracts depended on the phenolic concentration and composition. Sorghum with higher phenolic contents generally had higher inhibitory activity. Among the tested extracts, the brown sorghum (IS131C)-bran-free extract (BR-bran-free, half-maximal inhibitory concentration (IC50) = 18 ± 11 mg sorghum/mL) showed the strongest inhibition against α-glucosidase which was comparable to that of acarbose (IC50 = 1.39 ± 0.23 mg acarbose/mL). The red sorghum (Mr-Buster)-kernel-bound extract (RM-kernel-bound, IC50 = 160 ± 12 mg sorghum/mL) was the most potent in inhibiting α-amylase but was much weaker compared to acarbose (IC50 = 0.50 ± 0.03 mg acarbose/mL).

Synthesis and characterization of thermoresponsive diblock copolymer bearing amino acid moieties via click reaction

2011 ◽  
Vol 68 (5) ◽  
pp. 1315-1325 ◽  
Author(s):  
Zhilei Liu ◽  
Jianping Zhou ◽  
Hongbo Liang ◽  
Jianping Sun
Keyword(s):  
Amino Acid ◽  
Diblock Copolymer ◽  
Click Reaction ◽  
Synthesis And Characterization
Sign in / Sign up

Export Citation Format

Share Document