scholarly journals Asparagine-EDTA MNPs: A Highly Efficient And Recyclable Magnetic Multifunctional Core-Shell Nanocatalyst For Green Synthesis of Biologically-Active 3,4-Dihydropyrimidin-2(1H)-One Compounds

2021 ◽  
Author(s):  
Negin Rostami ◽  
Mohammad G Dekamin ◽  
Ehsan Valiey ◽  
Hamidreza FaniMoghadam
Keyword(s):  
Biginelli Reaction ◽  
Biologically Active ◽  
Catalyst Loading ◽  
Core Shell ◽  
Environmental Friendliness ◽  
Green Protocol ◽  
Highly Efficient ◽  
Solvent Free Conditions ◽  
Wide Range ◽  
Magnetic Stability

Abstract In this study, the new asparagine grafted on the EDTA-modified Fe3O4@SiO2 core-shell (Fe3O4@SiO2-APTS-EDTA-asparagine) magnetic nanoparticles were prepared and their structures were properly confirmed using different spectroscopic, microscopic and magnetic methods or techniques such as FT-IR, EDX, XRD, FESEM, TEM, TGA and VSM. The Fe3O4@SiO2-APTS-EDTA-asparagine core-shell nanomaterial was examined, as a highly efficient multifunctional and recoverable nanocatalyst, for the synthesis of a wide range of nitrogen-containing heterocycles and biologically-active 3,4-dihydropyrimidin-2(1H)-one derivatives under solvent-free conditions. It was proved that Fe3O4@SiO2-APTS-EDTA-asparagine MNPs, as a catalyst having excellent thermally and magnetic stability, specific morphology and acidic sites, can activate the Biginelli reaction components. Moreover, environmental-friendliness and nontoxic nature properties of the catalyst, cost effectiveness, low catalyst loading, easy separation of the catalyst from products and short time of reaction are some of the remarkable advantages of this green protocol.

scholarly journals Sulfamic acid pyromellitic diamide-functionalized MCM-41 as a multifunctional hybrid catalyst for melting-assisted solvent-free synthesis of bioactive 3,4-dihydropyrimidin-2-(1H)-ones

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Ehsan Valiey ◽  
Mohammad G. Dekamin ◽  
Zahra Alirezvani
Keyword(s):  
Structural Characteristics ◽  
Biginelli Reaction ◽  
High Surface ◽  
High Surface Area ◽  
Sulfamic Acid ◽  
Solvent Free ◽  
Biologically Active ◽  
Green Protocol ◽  
Solvent Free Conditions ◽  
Mcm 41

AbstractThis study introduces a practical approach to fabricate a novel hybrid acidic catalyst, namely sulfamic acid pyromellitic diamide-functionalized MCM-41 (MCM-41-APS-PMDA-NHSO3H). Various techniques such as FTIR, TGA, XRD, BET, FESEM, and EDX were used to confirm its structural characteristics. The efficiency of the new MCM-41-APS-PMDA-NHSO3H organosilica nanomaterials, as a heterogenous nanocatalyst, was examined in the synthesis of biologically active 3,4-dihydropyrimidin-2-(1H)-one derivatives under solvent-free conditions. It was found that the nanoporous MCM-41-APS-PMDA-NHSO3H, demonstrating acidic nature and high surface area, can activate all the Biginelli reaction components to afford desired 3,4-dihydropyrimidin-2-(1H)-ones under solvent-free conditions in short reaction time. Furthermore, easy and quick isolation of the new introduced hybrid organosilica from the reaction mixture as well as its reusability with negligible loss of activity in at least five consecutive runs are another advantages of this green protocol.

A highly efficient and green approach for the synthesis of pyrimido[4,5-b]quinolines using N,N-diethyl-N-sulfoethanaminium chloride

2021 ◽  
Vol 76 (2) ◽  
pp. 85-90
Author(s):  
Abdolkarim Zare ◽  
Manije Dianat
Keyword(s):  
Reaction Times ◽  
Solvent Free ◽  
One Pot ◽  
Catalyst Amount ◽  
Green Protocol ◽  
Highly Efficient ◽  
Green Approach ◽  
Solvent Free Conditions ◽  
The One ◽  
High Yields

Abstract A highly efficient and green protocol for the synthesis of pyrimido[4,5-b]quinolines has been described. The one-pot multicomponent reaction of dimedone with arylaldehydes and 6-amino-1,3-dimethyluracil in the presence of N,N-diethyl-N-sulfoethanaminium chloride ([Et3N–SO3H][Cl]) as an ionic liquid (IL) catalyst under solvent-free conditions afforded the mentioned compounds in high yields and short reaction times. Our protocol is superior to many of the reported protocols in terms of two or more of these factors: the reaction times, yields, conditions (solvent-free versus usage of organic solvents), temperature and catalyst amount.

Brønsted Acid-Catalysed Allylic Amination of 1-(2-Aminoaryl)prop-2-en-1-ols to 1,2-Dihydroquinolines

2018 ◽  
Vol 71 (9) ◽  
pp. 673 ◽  
Author(s):  
David Philip Day ◽  
Stuart Adam Henry ◽  
Yichao Zhao ◽  
Jianwen Jin ◽  
Guy James Clarkson ◽  
...  
Keyword(s):  
Room Temperature ◽  
Trifluoromethanesulfonic Acid ◽  
Catalyst Loading ◽  
Synthetic Method ◽  
Bronsted Acid ◽  
Allylic Amination ◽  
Mild Conditions ◽  
Highly Efficient ◽  
Brönsted Acid ◽  
Wide Range

A highly efficient synthetic method to prepare 1,2-dihydroquinolines that relies on trifluoromethanesulfonic acid (TfOH)-catalysed allylic amination of 1-(2-aminoaryl)prop-2-en-1-ols is described. Achieved at a catalyst loading of 0.01 mol-% under mild conditions at room temperature, the reaction was found to be robust, with a wide range of substitution patterns tolerated. The corresponding N-heterocyclic adducts were obtained in good to excellent yields of 45–93 %.

A highly efficient and green protocol for the synthesis of 3,3′-(arylmethylene)-bis(2-hydroxynaphthoquinone) derivatives catalyzed by a dicationic molten salt

2021 ◽  
Vol 76 (2) ◽  
pp. 91-95
Author(s):  
Abdolkarim Zare ◽  
Aysoda Ghobadpoor
Keyword(s):  
Molten Salt ◽  
Reaction Times ◽  
Solvent Free ◽  
Green Protocol ◽  
Highly Efficient ◽  
Solvent Free Conditions ◽  
High Yields

Abstract A highly efficient and green protocol for the synthesis of 3,3′-(arylmethylene)-bis(2-hydroxynaphthoquinone) {3,3′-(arylmethylene)-bis(2-hydroxynaphthalene-1,4-dione)} derivatives has been developed. The reaction of 2-hydroxynaphthoquinone (2-hydroxynaphthalene-1,4-dione) (2 eq.) and arylaldehydes (1 eq.) in the presence of the dicationic molten salt N,N,N′,N′-tetramethylethylenediaminium bis-hydrogensulfate ([TMEDAH2][HSO4]2) under solvent-free conditions afforded the mentioned compounds in high yields and relatively short reaction times.

Aspergillus sydowii Strain SCAU066 and Aspergillus versicolor Isolate BAB-6580: Potential Source of Xylanolytic, Cellulolytic and Amylolytic Enzymes

2020 ◽  
Vol 14 (2) ◽  
pp. 15
Author(s):  
Zaidah Zainal ariffin
Keyword(s):  
Extracellular Enzymes ◽  
Biologically Active ◽  
Aspergillus Versicolor ◽  
Aspergillus Sydowii ◽  
Aspergillus Tamarii ◽  
Alternative Source ◽  
Amylolytic Enzymes ◽  
Potato Dextrose Broth ◽  
Wide Range ◽  
Pharmaceutical Industries

Fungi is known to produce a wide range of biologically active metabolites and enzymes. Enzymes produced by fungi are utilized in food and pharmaceutical industries because of their rich enzymatic profile. Filamentous fungi are particularly interesting due to their high production of extracellular enzymes which has a large industrial potential. The aim of this study is to isolate potential soil fungi species that are able to produce functional enzymes for industries. Five Aspergillus species were successfully isolated from antibiotic overexposed soil (GPS coordinate of N3.093219 E101.40269) by standard microbiological method. The isolated fungi were identified via morphological observations and molecular tools; polymerase chain reactions, ITS 1 (5’- TCC GTA GGT GAA CCT GCG G3’) forward primer and ITS 4 (5’-TCC TCC GCT TAT TGA TAT GC-3’) reverse primer. The isolated fungi were identified as Aspergillus sydowii strain SCAU066, Aspergillus tamarii isolate TN-7, Aspergillus candidus strain KUFA 0062, Aspergillus versicolor isolate BAB-6580, and Aspergillus protuberus strain KAS 6024. Supernatant obtained via submerged fermentation of the isolated fungi in potato dextrose broth (PDB) and extracted via centrifugation was loaded onto specific media to screen for the production of xylanolytic, cellulolytic and amylolytic enzymes. The present findings indicate that Aspergillus sydowii strain SCAU066 and Aspergillus versicolor isolate BAB-6580 have great potential as an alternative source of xylanolytic, cellulolytic and amylolytic enzymes.

Nickel(0)-Catalyzed Linear-Selective Hydroarylation of Unactivated Alkenes and Styrenes with Arylboron Acids

2018 ◽  
Author(s):  
Honggui Lv ◽  
Li-Jun Xiao ◽  
Dongbing Zhao ◽  
Qi-Lin Zhou
Keyword(s):  
Butyric Acid ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Highly Efficient ◽  
Organoboronic Acids

Herein, we realized the first linear-selective hydroarylation of unactivated alkenes and styrenes with organoboronic acids by introducing directing groupon alkenes. Our method is highly efficient and scalable, and provides a modular route to assemble structurally diverse alkylarenes, especially for γ-aryl butyric acid derivatives, which have been widely utilized as chemical feedstocks to access multiple marketed drugs, and biologically active compounds.<br>

One-Dimensional TiO2@GaON Core-Shell Nanowires with Controlled Shell Thickness from Atomic Layer Deposition for Stable and Efficient Photoelectrochemical Water Splitting

2019 ◽  
Author(s):  
Jiajia Tao ◽  
Hong-Ping Ma ◽  
Kaiping Yuan ◽  
Yang Gu ◽  
Jianwei Lian ◽  
...  
Keyword(s):  
Atomic Layer Deposition ◽  
Band Gap ◽  
Water Splitting ◽  
Atomic Layer ◽  
Photoelectrochemical Water Splitting ◽  
Core Shell ◽  
Photoelectrochemical Performance ◽  
Highly Efficient ◽  
Layer Deposition ◽  
Shell Nanowires

<div>As a promising oxygen evolution reaction semiconductor, TiO2 has been extensively investigated for solar photoelectrochemical water splitting. Here, a highly efficient and stable strategy for rationally preparing GaON cocatalysts on TiO2 by atomic layer deposition is demonstrated, which we show significantly enhances the</div><div>photoelectrochemical performance compared to TiO2-based photoanodes. For TiO2@20 nm-GaON core-shell nanowires a photocurrent density up to 1.10 mA cm-2 (1.23 V vs RHE) under AM 1.5 G irradiation (100 mW cm-2) has been achieved, which is 14 times higher than that of TiO2 NWs. Furthermore, the oxygen vacancy formation on GaON as well as the band gap matching with TiO2 not only provides more active sites for water oxidation but also enhances light absorption to promote interfacial charge separation and migration. Density functional theory studies of model systems of GaON-modified TiO2 confirm the band gap reduction, high reducibility and ability to activate water. The highly efficient and stable systems of TiO2@GaON core-shell nanowires provide a deeper understanding and universal strategy for enhancing photoelectrochemical performance of photoanodes now available. </div>

The content of decenoic acids in drone brood preparations and combined preparations based on it

Biomics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 389-393
Author(s):  
D.V. Mitrofanov ◽  
N.V. Budnikova
Keyword(s):  
Royal Jelly ◽  
Storage Conditions ◽  
Water Soluble ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Strict Adherence ◽  
Drone Brood ◽  
Wide Range ◽  
Active Substances ◽  
Melanin Complex

The drone brood contains a large number of substances with antioxidant activity. These substances require stabilization and strict adherence to storage conditions. Among these substances are unique decenoic acids, the content of which is an indicator of the quality of drone brood and products based on it. The ability of drone brood to reduce the manifestations of oxidative stress is shown. There are dietary supplements for food and drugs based on drone brood, which are used for a wide range of diseases. Together with drone brood, chitosan-containing products, propolis, royal jelly can be used. They enrich the composition with their own biologically active substances and affect the preservation of the biologically active substances of the drone brood. Promising are the products containing, in addition to the drone brood, a chitin-chitosan-melanin complex from bees, propolis, royal jelly. The chitin-chitosan-melanin complex in the amount of 5% in the composition of the adsorbent practically does not affect the preservation of decenic acids, while in the amount of 2% and 10% it somewhat worsens. The acid-soluble and water-soluble chitosan of marine crustaceans significantly worsens the preservation of decenoic acids in the product. Drone brood with royal jelly demonstrates a rather high content of decenoic acids. When propolis is introduced into the composition of the product, the content of decenoic acids increases according to the content of propolis.

Privileged Structures in the Design of Potential Drug Candidates for Neglected Diseases

2019 ◽  
Vol 26 (23) ◽  
pp. 4323-4354 ◽  
Author(s):  
Ana Cristina Lima Leite ◽  
José Wanderlan Pontes Espíndola ◽  
Marcos Veríssimo de Oliveira Cardoso ◽  
Gevanio Bezerra de Oliveira Filho
Keyword(s):  
Biologically Active ◽  
Neglected Diseases ◽  
Financial Return ◽  
Drug Candidates ◽  
Lead Compounds ◽  
Wide Range ◽  
Methods Of Synthesis ◽  
Current Therapies ◽  
Resistant Strains ◽  
Privileged Structures

Background: Privileged motifs are recurring in a wide range of biologically active compounds that reach different pharmaceutical targets and pathways and could represent a suitable start point to access potential candidates in the neglected diseases field. The current therapies to treat these diseases are based in drugs that lack of the desired effectiveness, affordable methods of synthesis and allow a way to emergence of resistant strains. Due the lack of financial return, only few pharmaceutical companies have been investing in research for new therapeutics for neglected diseases (ND). Methods: Based on the literature search from 2002 to 2016, we discuss how six privileged motifs, focusing phthalimide, isatin, indole, thiosemicarbazone, thiazole, and thiazolidinone are particularly recurrent in compounds active against some of neglected diseases. Results: It was observed that attention was paid particularly for Chagas disease, malaria, tuberculosis, schistosomiasis, leishmaniasis, dengue, African sleeping sickness (Human African Trypanosomiasis - HAT) and toxoplasmosis. It was possible to verify that, among the ND, antitrypanosomal and antiplasmodial activities were between the most searched. Besides, thiosemicarbazone moiety seems to be the most versatile and frequently explored scaffold. As well, phthalimide, isatin, thiazole, and thiazolidone nucleus have been also explored in the ND field. Conclusion: Some described compounds, appear to be promising drug candidates, while others could represent a valuable inspiration in the research for new lead compounds.

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