scholarly journals Microwave assisted green synthesis of pharmaceutically potent benzoxanthone analogues employing biodegradable oxalic acid as ecofriendly catalyst

2019 ◽  
Vol 9 (5) ◽  
pp. 4311-4316
Keyword(s):  
Oxalic Acid ◽  
Research Work ◽  
Aromatic Aldehydes ◽  
Water Medium ◽  
Spectroscopic Techniques ◽  
Green Catalyst ◽  
Green Approach ◽  
Microwave Irradiations ◽  
Ft Ir ◽  
Good Percentage

The aim of the present research work is to develop an efficient and ecofriendly methodology to synthesize benzoxanthones analogs by employing oxalic acid as nontoxic, biodegradable catalyst in water medium. The reactions were carried out under microwave irradiations. Thus hereby a series of benzoxanthones were synthesized from various aromatic aldehydes of varying electronic natures via a complete green approach where microwave irradiation was used as an efficient green source of energy, oxalic acid was employed as green catalyst and water were used as green solvent in all the reactions. The synthesized compounds have given a good percentage of yield of all the products and they were characterized by melting point, FT-IR, H1-NMR C13-NMR and mass spectroscopic techniques.

scholarly journals SYNTHESIS AND ANTIMALARIAL ACTIVITY OF SOME NEW 3-PHENYL-2-THIOXOTHIAZOLIDIN-4-ONE DERIVATIVES

2017 ◽  
Vol 9 (3) ◽  
pp. 58
Author(s):  
Mehul Zaveri ◽  
Neha Kawathekar
Keyword(s):  
Antimalarial Activity ◽  
Research Work ◽  
Aromatic Aldehydes ◽  
Maximum Activity ◽  
Spectroscopic Techniques ◽  
Activity Data ◽  
Antimalarial Agents ◽  
Ic50 Values ◽  
Current Therapies

Objective: Current therapies to treat P. falciparum malaria are heavily reliant on artemisinin-based combinations. However, resistance to artemisinin has recently been identified, and resistance to key artemisinin partner drugs is already widespread. Therefore, there is an urgent need for new antimalarial drugs with improved attributes over older therapies. The objective of this research work is to synthesize new antimalarial agents more effective against clinically relevant malarial strains.Methods: In present work, a series of ten 3-phenyl-2-thioxothiazolidin-4-one (MF1-MF10) derivatives, were synthesized by Knoevenagel condensation of N-phenyl rhodanine (I1) with substituted aromatic or hetro aromatic aldehydes using microwave irradiation. N-phenyl rhodanine (I1) was synthesized by a conventional reaction involving methyl-2-mercaptoacetate (1) and phenyl Isothiocyanates in presence of triethylamine. All the synthesized compounds were characterized by various spectroscopic techniques and evaluated for in-vitro antimalarial activity by microdilution technique against resistance strains of Plasmodium falciparum.Results: The antimalarial activity data showed that six compounds (MF1, MF3, MF4, MF5, MF7 and MF8) exhibited IC50 values ranging from 1.0-1.30 µg/ml, three compounds (MF2, MF6 and MF10) displayed IC50 values in the range of 0.9-1.0 µg/ml. Compound MF9 showed most significant result with maximum activity (IC50 = 0.85µg/ml).Conclusion: The antimalarial activity results revealed that compound MF9 possess potent activity and could be identified as a promising lead for further investigation.

Synthesis and Molecular Docking Studies of (E)-4-(Substituted-benzylideneamino)-2H-Chromen-2-one Derivatives: Entry to New Carbonic Anhydrase Class Of Inhibitors

Drug Research ◽  
2018 ◽  
Vol 68 (07) ◽  
pp. 378-386 ◽  
Author(s):  
Tanzeela Fattah ◽  
Aamer Saeed ◽  
Pervaiz Channar ◽  
Fayaz Larik ◽  
Mubashir Hassan ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Carbonic Anhydrase ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Aromatic Aldehydes ◽  
Docking Studies ◽  
Spectroscopic Techniques ◽  
Amino Acid Residues ◽  
Drug Score ◽  
Ft Ir

The present article illustrated the synthesis and characterization of a novel series of (E)-4-(substituted-benzylideneamino)-2H-chromen-2-one derivatives 4a-4j in good to excellent yields. The target compounds were synthesized by refluxing 4-aminocoumarin with aromatic aldehydes in ethanol. The structural confirmation was achieved by spectroscopic techniques such as (1H, 13C-NMR and FT-IR) and elemental analysis. The synthesized compounds were evaluated for carbonic anhydrase II (CA-II) inhibition and free radical scavenging activity. All the compounds showed CA-II inhibition in the micro molar range. The compound 4c exhibited higher potential in the series with IC50=0.0928±0.00545 µM (standard Acetazolamide IC50=0.997±0.0586 µM). Pharmacological investigations showed that the synthesized compounds 4a-4j obey Lipinsk’s rule. Compound 4c elicited drug likeness and showed drug score value of 0.05. Molecular docking analysis showed that compound 4c interacts with Asn66 and Gln91 amino acid residues. Graphical Abstract.

scholarly journals A Green Approach to the Production of 2-pyridone Derivatives Promoted by Infrared Irradiation

2017 ◽  
Vol 58 (2) ◽  
Author(s):  
Fernando Hernández ◽  
Fabiola De la Cruz ◽  
Julio López ◽  
Eduardo Peña ◽  
Francisco Delgado ◽  
...  
Keyword(s):  
Spectroscopic Techniques ◽  
Infrared Irradiation ◽  
X Ray Diffraction ◽  
Reaction Conditions ◽  
X Ray ◽  
H Nmr ◽  
Green Approach ◽  
Ft Ir ◽  
Target Molecules ◽  
C Nmr

<p>An alternative is presented for promoting a reaction with infrared irradiation to obtain different 4-aryl-3-cyano-5-ethoxycarbonyl-6-methyl-2-pyridone derivatives <strong>9a-k</strong>. The process was carried out with a green approach from the corresponding 4<em>H</em>-pyrans, using mild reaction conditions and infrared irradiation as the energy source. In the first stage, the reaction produced 1,2,3,4-tetrahydropyridin-2-one derivatives <strong>8a-k</strong>, followed by an oxidative step to afford the target molecules in good yields. The structure of products <strong>9a-k</strong> was confirmed by FT-IR, <sup>1</sup>H NMR and <sup>13</sup>C NMR spectroscopic techniques and X-ray diffraction. It was found that the efficiency of the reaction depends on the catalyst and the solvent, as well as on the aldehyde substituents.</p>

Solubility Enhancement of Poorly Water-Soluble Antifungal Drug Acyclovir by Nanocrystal Formulation Approach

2018 ◽  
Vol 11 (2) ◽  
pp. 4036-4042
Author(s):  
Prakash Goudanavar ◽  
Ankit Acharya ◽  
Vinay C.H
Keyword(s):  
Chemical Interaction ◽  
Research Work ◽  
Antiviral Drug ◽  
In Vitro Release ◽  
Oral Route ◽  
Water Soluble ◽  
Precipitation Method ◽  
Dsc Studies ◽  
Ft Ir

Administration of an antiviral drug, acyclovir via the oral route leads to low and variable bioavailability (15-30%). Therefore, this research work was aimed to enhance bioavailability of acyclovir by nanocrystallization technique. The drug nanocrystals were prepared by anti-solvent precipitation method in which different stabilizers were used. The formed nanocrystals are subjected to biopharmaceutical characterization including solubility, particle size and in-vitro release. SEM studies showed nano-crystals were crystalline nature with sharp peaks. The formulated drug nanocrystals were found to be in the range of 600-900nm and formulations NC7 and NC8 showed marked improvement in dissolution velocity when compared to pure drug, thus providing greater bioavailability. FT-IR and DSC studies revealed the absence of any chemical interaction between drug and polymers used. 

Zinc Sulfamate Catalyzed Efficient Selective Synthesis of Benzimidazole Derivatives under Ambient Conditions

2019 ◽  
Vol 16 (9) ◽  
pp. 740-749
Author(s):  
Sushil R. Mathapati ◽  
Arvind H. Jadhav ◽  
Mantosh B. Swami ◽  
Jairaj K. Dawle
Keyword(s):  
Benzimidazole Derivative ◽  
Sulfamic Acid ◽  
Aromatic Aldehydes ◽  
Catalytic Amount ◽  
Product Yield ◽  
Lewis Acidity ◽  
Benzimidazole Derivatives ◽  
Ambient Conditions ◽  
Reaction Condition ◽  
Green Approach

Zinc sulfamate (Zn(NH2SO3)2 is a derivative of sulfamic acid (H3NSO3) which possesses “Lewis acidity” and finds well suited in a number of catalytic applications. The present paper describes an efficient, eco-friendly, and clean synthesis of 2-substituted benzimidazole derivatives by reacting diverse o-phenylenediamine with various substituted aromatic aldehydes using a catalytic amount of zinc sulfamate in ethanol at ambient temperature. As a result, 10 mol.% of Zinc sulfamate catalyst showed 92% of respective product yield with 100% conversion using short reaction period in ethanol. Meanwhile, effect of reaction parameters, such as amount of catalyst, different solvents, and reaction temperature on reaction product, was also studied. In addition, in the optimized reaction condition various substituted biological important benzimidazoles derivatives were prepared by using optimized reaction condition in good to efficient yield. In addition, possible reaction mechanism in the presence of zinc sulfamate for the preparation of benzimidazole derivative was sketched and discussed. The present green approach showed significances with faster reaction rate with inexpensive catalyst, which showed excellent and clean yield of benzimidazole in mild reaction condition with easy work-up procedure.

Synthesis, Characterization and Application of N,N-Dimethyl-N-Sulfoethan Ammonium tetra-Chloro Aluminate: A Novel micro-Heterogeneous Cata-lyst for Synthesis of tri-Arylmethanes

2020 ◽  
Vol 17 ◽  
Author(s):  
Saeid Azimi ◽  
Niloofar Mohamadighader
Keyword(s):  
Ionic Liquid ◽  
Heterogeneous Catalyst ◽  
Mass Spectroscopy ◽  
Aromatic Aldehydes ◽  
Solid Catalyst ◽  
Sem Images ◽  
One Pot ◽  
Acidic Catalyst ◽  
Eds Analysis ◽  
Ft Ir

Abstract: A new solid catalyst was synthesized from an ionic liquid and heterogenised by changing anion reaction. The new heterogeneous acidic catalyst was characterized by SEM images, EDS analysis, AFM images, Ft-IR, HNMR, 13CNMR and Mass Spectroscopy. It was applied to synthesis of tri-arylmethanes throughout one-pot tri-component reactions among aromatic aldehydes, N,N-dimethylaniline and other carbonic nucleophiles such as anisole and indole. Hence, synthesis of convenient and inexpensive micro-heterogeneous catalyst was introduced, the efficiency of which was confirmed. Also, various useful products were synthesized throughout this simple and clean procedure.

SO3H-functionalized Zeolite-Y as an Efficient Nanocatalyst for the Synthesis of Nbenzimidazole- 2-aryl-4-thiazolidinones and tri-substituted Imidazoles

2020 ◽  
Vol 17 (2) ◽  
pp. 117-130 ◽  
Author(s):  
Mehdi Kalhor ◽  
Zohre Zarnegar ◽  
Zahra Seyedzade ◽  
Soodabeh Banibairami
Keyword(s):  
Zeolite Y ◽  
Internal Standard ◽  
Acid Catalyst ◽  
Aromatic Aldehydes ◽  
Reaction Rates ◽  
Ambient Conditions ◽  
Catalytic Method ◽  
Efficient Catalyst ◽  
Bet Analysis ◽  
Ft Ir

Background: SO3H-functionalized zeolite-Y was prepared and used as a catalyst for the synthesis of 2-aryl-N-benzimidazole-4-thiazolidinones and tri-substituted imidazoles at ambient conditions. Objective: The goals of this catalytic method include excellent yields and high purity, inexpensive procedure and ease of product isolation, the use of nontoxic and heterogeneous acid catalyst, shorter reaction times and milder conditions. Materials and Methods: NMR spectra were recorded on Brucker spectrophotometer using Me4Si as internal standard. Mass spectra were recorded on an Agilent Technology 5975C VL MSD with tripe-axis detector. FTIR spectra were obtained with KBr disc on a galaxy series FT-IR 5000 spectrometer. The surface morphology of nanostructures was analyzed by FE-SEM (EVO LS 10, Zeiss, Carl Zeiss, Germany). BET analysis were measured at 196 °C by a Japan Belsorb II system after the samples were vacuum dried at 150°C overnight. Results: The NSZ was characterized by FT-IR, FESEM, EDX, XRF, and BET. The catalytic activity of NSZ was investigated for synthesis of 1,3-tiazolidin-4-ones in H2O/Acetone at room temperature. Moreover, NSZ was used for synthesis of tri-substituted imidazoles at 60 °C via solvent-free condensation. Different kinds of aromatic aldehydes were converted to the corresponding of products with good to excellent yields. Conclusion: Sulfonated zeolite-Y was as an efficient catalyst for the preparation of N-benzimidazole-2-aryl-1,3- thiazolidin-4-ones and 2,4,5-triaryl-1H-imidazoles. High reaction rates, elimination toxic solvent, simple experimental procedure and reusability of the catalyst are the important features of this protocol.

Ultrasound-assisted aqua-mediated synthesis of multi-substituted tetrahydropyridine-3-carboxylates using N-carboxymethyl-3-pyridinium hydrogensulfate ([N-CH2CO2H-3-pic]+HSO4−) as a new efficient ionic liquid catalyst

2021 ◽  
Vol 3 (6) ◽  
Author(s):  
Kobra Nikoofar ◽  
Fatemeh Shahriyari
Keyword(s):  
Ionic Liquid ◽  
Reaction Times ◽  
Aromatic Aldehydes ◽  
Environmentally Benign ◽  
H Nmr ◽  
Sonic Waves ◽  
Ft Ir ◽  
High Yields ◽  
Work Up ◽  
C Nmr

AbstractA simple, straightforward, and ultrasound-promoted method for the preparation of some highly functionalized tetrahydropyridines reported via pseudo five-component reaction of (hetero)aromatic aldehydes, different anilines, and alkyl acetoacetates in the presence of [N-CH2CO2H-3-pic]+HSO4−, as a novel ionic liquid, in green aqueous medium. The IL was synthesized utilizing simple and easily-handled substrates and characterized by FT-IR, 1H NMR, 13C NMR, GC-MASS, FESEM, EDX, and TGA/DTG techniques. The procedure contains some highlighted aspects which are: (a) performing the MCR in the presence of aqua and sonic waves, as two main important and environmentally benign indexes in green and economic chemistry, (b) high yields of products within short reaction times, (c) convenient work-up procedure, (d) preparing the new IL via simple substrates and procedure.

scholarly journals Synthesis and Bioinformatic Characterization of New Schiff Bases with Possible Applicability in Brain Disorders

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4160
Author(s):  
Speranta Avram ◽  
Ana Maria Udrea ◽  
Diana Camelia Nuta ◽  
Carmen Limban ◽  
Adrian Cosmin Balea ◽  
...  
Keyword(s):  
Schiff Bases ◽  
Neurodegenerative Disorders ◽  
Aromatic Aldehydes ◽  
Brain Disorders ◽  
Ir And Nmr Spectroscopy ◽  
Bioinformatics Tools ◽  
Ft Ir ◽  
New Treatments ◽  
New Compounds

(1) Background: The research aims to find new treatments for neurodegenerative diseases, in particular, Alzheimer’s disease. (2) Methods: This article presents a bioinformatics and pathology study of new Schiff bases, (EZ)-N′-benzylidene-(2RS)-2-(6-chloro-9H-carbazol-2-yl)propanehydrazide derivatives, and aims to evaluate the drug-like, pharmacokinetic, pharmacodynamic and pharmacogenomic properties, as well as to predict the binding to therapeutic targets by applying bioinformatics, cheminformatics and computational pharmacological methods. (3) Results: We obtained these Schiff bases by condensing (2RS)-2-(6-chloro-9H-carbazol-2-yl)propanehydrazide with aromatic aldehydes, using the advantages of microwave irradiation. The newly synthesized compounds were characterized spectrally, using FT-IR and NMR spectroscopy, which confirmed their structure. Using bioinformatics tools, we noticed that all new compounds are drug-likeness features and may be proposed as potentially neuropsychiatric drugs (4) Conclusions: Using bioinformatics tools, we determined that the new compound 1e had a high potential to be used as a good candidate in neurodegenerative disorders treatment.

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