scholarly journals Synthesis and Heme Polymerization Inhibitory Activity (HPIA) Assay of Antiplasmodium of (1)-N-(3,4-Dimethoxybenzyl)-1,10-Phenanthrolinium Bromide from Vanillin

2014 ◽  
Vol 14 (1) ◽  
pp. 1-6
Author(s):  
Dhina Fitriastuti ◽  
Muhammad Idham Darussalam Mardjan ◽  
Jumina Jumina ◽  
Mustofa Mustofa
Keyword(s):  
Melting Point ◽  
Sodium Borohydride ◽  
Inhibitory Activity ◽  
Veratryl Alcohol ◽  
Activity Assay ◽  
Light Yellow ◽  
Grinding Method ◽  
Methylation Product ◽  
Ft Ir ◽  
Phenanthroline Monohydrate

The synthesis of (1)-N-(3,4-dimethoxy-benzyl)-1,10-phenanthrolinium bromide had been conducted from vanillin. Heme polymerization inhibitory activity assay of the synthesized antiplasmodium has also been carried out. The first step of reaction was methylation of vanillin using dimethylsulfate and NaOH. The mixture was refluxed for 2 h to yield veratraldehyde in the form of light yellow solid (79% yield). Methylation product was reduced using sodium borohydride (NaBH4) with grinding method and yielded veratryl alcohol in the form of yellow liquid (98% yield). Veratryl alcohol was brominated using PBr3 to yield yellowish black liquid (85% yield). The final step was benzylation of 1,10-phenanthroline monohydrate with the synthesized veratryl bromide under reflux condition in acetone for 14 h to afford (1)-N-(3,4-dimethoxy-benzyl)-1,10-phenanthrolinium bromide (84%) as yellow solid with melting point of 166-177 °C. The structures of products were characterized by FT-IR, GC-MS and 1H-NMR spectrometers. The results of heme polymerization inhibitory activity assay of (1)-N-(3,4-dimethoxybenzyl)-1,10-phenanthrolinium bromide showed that it had IC50 HPIA of 3.63 mM, while chloroquine had IC50 of4.37 mM. These results indicated that (1)-N-(3,4-dimethoxybenzyl)-1,10-phenanthrolinium bromide was more potential antiplasmodium than chloroquine.

scholarly journals SYNTHESIS AND ANTIPLASMODIAL ACTIVITY TESTING OF (1)-N-(4-METHOXYBENZYL)-1,10-PHENANTHROLINIUM BROMIDE

2010 ◽  
Vol 7 (2) ◽  
pp. 197-201 ◽  
Author(s):  
Ruslin Hadanu ◽  
Sabirin Mastjeh ◽  
Jumina Jumina ◽  
Mustofa Mustofa ◽  
Mahardika Agus Widjayanti ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Melting Point ◽  
1H Nmr ◽  
Sodium Borohydride ◽  
Starting Material ◽  
Antiplasmodial Activity ◽  
Microscopic Method ◽  
Phenanthroline Monohydrate ◽  
Solid Form

Synthesis of (1)-N-(4-methoxybenzyl)-1,10-phenanthroline bromide from 1,10-phenanthroline monohydrate and 4-methoxybenzaldehyde as starting material and evaluation of its antiplasmodial activities have been carried out. The 4-methoxybenzyl alcohol was prepared from 4-methoxy-benzaldehyde using sodium borohydride (NaBH4) reagent and ethanol absolute solution. The mixture was refluxed for 3 h. To yield colorless dilution compound with 90.41 % in efficiency. Furthermore, bromination of 4-methoxybenzyl alcohol with phosphorus bromide (PBr3) was conducted by refluxing for 3 h. The product of this reaction was yellow liquid of 4-methoxybenzyl bromide, 79.03% yield and 95.34 % purity. The final step of reaction was benzylation of 1,10-phenanthroline monohydrate with 4-methoxybenzyl bromide reagent. It was conducted by refluxing in aceton for 8 h at 55 oC. The yield of the reaction was (1)-N-(4-methoxybenzyl)-1,10-phenanthroline bromide (77.63%). It is pink solid form, and its melting point is 192-193 oC. Identification of the product was carried out by means of GC-MS, IR and 1H-NMR spectrometers. The in vitro antiplasmodial activity on chloroquine-resistant Plasmodium falciparum FCR-3 strain and chloroquine sensitive P. falciparum D10 strain for (1)-N-(4-methoxybenzyl)-1,10-phenanthroline bromide were determined by microscopic method. The result showed that after 72 h incubation, it has IC50 0.93±0.02 µM and 1.21±0.09 µM, respectively.   Keywords: 1,10-phenanthroline,  (1)-N-(4-methoxybenzyl)-1,10-phenanthroline bromide, 4 methoxybenzaldehyde, antiplasmodial activities

Synthesis N-Phenyl Pyrazoline from Dibenzalacetone and Heme Polymeration Inhibitory Activity (HPIA) Assay

2020 ◽  
Vol 840 ◽  
pp. 245-250
Author(s):  
Linda Ekawati ◽  
Bambang Purwono ◽  
Muhammad Idham Darussalam Mardjan
Keyword(s):  
Acetic Acid ◽  
Inhibitory Activity ◽  
Activity Assay ◽  
Ft Ir ◽  
Benzaldehyde Derivatives ◽  
C Nmr

The synthesis of 1,5-diphenyl-3-styryl-4,5-dihydro-1H-pyrazole (B1) and 5-(3,4-dimethoxyphenyl)-3-(3,4-dimethoxystyryl)-1-phenyl-4,5-dihydro-1H-pyrazole (B2) have been conducted from 1,5-diphenylpenta-1,4-dien-3-on (A1) and 1,5-bis(3,4-dimethoxyphenyl)penta-1,4-dien-3-one (A2). Heme polymerization inhibitory activity (HPIA) assay of the synthesized compounds has also been carried out. The first step of reaction was Claisen-Schmidt condensation of benzaldehyde derivatives and acetone using NaOH 20% and ethanol as solvent. Dibenzalacetone derivatives were reacted with phenylhydrazine using acetic acid to form N-phenylpyrazoline. The structure of products was characterized by FT-IR, GC-MS, DI-MS, 1H- and 13C-NMR The result of heme polymerization inhibitory activity assay showed that IC50 of B1 and B2 1.26 and 0.79 mM while quinine 1.26 mM. The result indicated that compound B2 was more potent as antimalarial than quinine.

Preparation and Photocatalytic Activity of Cu/BiVO4 by Solid State Grinding Method for Degradation of Methyl Orange

2016 ◽  
Vol 703 ◽  
pp. 321-325
Author(s):  
Hai Feng Chen ◽  
Jia Mei Chen ◽  
Zhi Xue Pan
Keyword(s):  
Methyl Orange ◽  
Solid State ◽  
Visible Light ◽  
Raw Materials ◽  
X Ray Diffraction ◽  
Visible Absorption ◽  
Illumination Time ◽  
Grinding Method ◽  
Ft Ir ◽  
Degradation Of Methyl Orange

In this work, novel Cu/BiVO4 photocatalyst were prepared by a low-temperature solid state grinding method using Bi (NO3)3•5H2O, NH4VO3 and Cu (NO3)2•2H2O as raw materials. The structure and properties of the samples were characterized by Infrared Spectroscopy (FT-IR), X-ray diffraction (XRD) and UV-vis diffused reflectance spectroscopy (DRS); Using the degradation of methyl orange (MO) as the probe, it was simulated as the degradation of sewage under the visible light to study the influence of the illumination time and the amount of photocatalysts. Compared with the pure BiVO4, the visible-light absorption scope of BiVO4 was broadened by doping Cu, the UV-Visible absorption edges were slightly red shift and the band gap was narrower. Comparatively speaking, the results indicted that the doped Cu enhanced the photocatalytic activities of BiVO4.

scholarly journals Quinazolin-4(3H)-ones and 5,6-Dihydropyrimidin-4(3H)-ones from β-Aminoamides and Orthoesters

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2925 ◽  
Author(s):  
Joshua Gavin ◽  
Joel Annor-Gyamfi ◽  
Richard Bunce
Keyword(s):  
Acetic Acid ◽  
Melting Point ◽  
1H Nmr ◽  
13C Nmr ◽  
Pressure Tube ◽  
Absolute Ethanol ◽  
Basic Nitrogen ◽  
One Step ◽  
Ft Ir

Quinazolin-4(3H)-ones have been prepared in one step from 2-aminobenzamides and orthoesters in the presence of acetic acid. Simple 2-aminobenzamides were easily converted to the heterocycles by refluxing in absolute ethanol with 1.5 equivalents of the orthoester and 2 equivalents of acetic acid for 12–24 h. Ring-substituted and hindered 2-aminobenzamides as well as cases incorporating an additional basic nitrogen required pressure tube conditions with 3 equivalents each of the orthoester and acetic acid in ethanol at 110 °C for 12–72 h. The reaction was tolerant towards functionality on the benzamide and a range of structures was accessible. Workup involved removal of the solvent under vacuum and either recrystallization from ethanol or trituration with ether-pentane. Several 5,6-dihydropyrimidin-4(3H)-ones were also prepared from 3-amino-2,2-dimethylpropionamide. All products were characterized by melting point, FT-IR, 1H-NMR, 13C-NMR, and HRMS.

scholarly journals Betalains in Edible Fruits of Three Cactaceae Taxa—Epiphyllum, Hylocereus, and Opuntia—Their LC-MS/MS and FTIR Identification and Biological Activities Evaluation

Plants ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 2669
Author(s):  
Michaela Barkociová ◽  
Jaroslav Tóth ◽  
Katarzyna Sutor ◽  
Natalia Drobnicka ◽  
Slawomir Wybraniec ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antioxidant Activity ◽  
Food Industry ◽  
Biological Activities ◽  
Ornamental Plants ◽  
Reducing Power ◽  
Activity Assay ◽  
Natural Pigment ◽  
E Coli ◽  
Ft Ir

Epiphyllum, Hylocereus, and Opuntia plants belong to the Cactaceae family. They are mostly known as ornamental plants but also for their edible fruits, which can potentially be sources of betalains, such as betanin, a natural pigment used in the food industry, e.g., under the European label code E 162. The aim of this work was the identification of betalains (using LC-MS/MS), evaluation of total betalain content (spectrophotometrically), analysis of functional groups (using FT-IR), evaluation of antioxidant activity (using DPPH, ABTS, FRAP, DCFH-DA, and reducing power methods) and evaluation of antimicrobial activity (S. aureus, E. coli, and C. albicans) in fruits of Epiphyllum, Hylocereus, and Opuntia taxa. A total of 20 betalains were identified in the studied Cactaceae fruits. The Epiphyllum pink hybrid had the highest values of total betalains amongst all samples. The highest antioxidant activity was observed in the Epiphyllum pink hybrid, in Opuntia zacuapanensis and O. humifusa fruits. The antimicrobial activity assay showed that cacti fruits were not able to effectively inhibit the growth of E. coli, S. aureus, or C. albicans. Our results prove that these fruits are good sources of natural pigments—betalains. They do not contain toxic compounds in significant amounts and they exhibit antioxidant activity.

scholarly journals Synthesis of Cinnamic Acid Based on Perkin Reaction Using Sonochemical Method and Its Potential as Photoprotective Agent

2020 ◽  
Vol 5 (1) ◽  
pp. 54
Author(s):  
Erwin Indriyanti ◽  
Masitoh Suryaning Prahasiwi
Keyword(s):  
Antioxidant Activity ◽  
Melting Point ◽  
Cinnamic Acid ◽  
Wave Number ◽  
Sonochemical Method ◽  
H Nmr ◽  
Ft Ir ◽  
Perkin Reaction ◽  
Pharmaceutical Industries ◽  
C Nmr

<p>Cinnamic acid plays a vital role in the synthesis of other important compounds and as a precursor for the synthesis of commercial cinnamon esters used in perfumery, cosmetics, and pharmaceutical industries. The aim of this research is to synthesize cinnamic acid using sonochemical methods. Cinnamic acid was synthesized using Perkin reaction by reacting 0.05 mole of benzaldehyde with 0.073 mole of acetic acid anhydride and 0.03 mole of sodium acetate as a catalyst in the Erlenmeyer flask and then the mixture was put in a sonicator for 60 minutes at 70 <sup>o</sup>C. The synthesized compound was tested organoleptic properties, and the melting point was measured. The chemical structure was elucidated using FT-IR, H-NMR, and <sup>13</sup>C-NMR. The photoprotective activity was examined from its antioxidant and SPF values. The synthesized compound was found in the form of a shiny white fine crystal which had distinctive odor with a yield of 4.98% and the melting point was found at 133<sup> o</sup>C. In the structure elucidation using FT-IR (the aromatic ring absorption at the wave number 1580 cm<sup>-1</sup> -1600 cm<sup>-1</sup>. The wave number 1625 cm<sup>-1</sup>is an aromatic conjugated alkene group, while wave  number 1689.4 cm<sup>-1 </sup>is a carbonyl group. The wave number 2500 cm<sup>-1 </sup>– 3250 cm<sup>-1 </sup>is an OH carboxylic acid group) , H-NMR (7.410 (<em>m</em>, 5H, Ar-H); 7.425(<em>t</em>, 1H); 7.572 (<em>d</em>, 1H); 8.057 (d, 1H,C=CH) and <sup>13</sup>C-NMR (129.309 ppm; 130.998 ppm; 134.58 ppm; 170.017 ppm) showed that when compared with the standard compound as the reference, the synthesized compound was confirmed to be cinnamic acid. The antioxidant activity test showed that at the concentration of 20 ppm the synthesized compound was able to reduce free radicals by 46.69%. This finding showed that  the synthesized compound had antioxidant activity.</p>

scholarly journals Synthesis of N-benzothiazole derivative imide on polymeric chain, have possible biological activity

2013 ◽  
Vol 10 (3) ◽  
pp. 673-685
Author(s):  
Baghdad Science Journal
Keyword(s):  
Thermal Analysis ◽  
Biological Activity ◽  
Melting Point ◽  
13C Nmr ◽  
Uv Spectroscopy ◽  
Polymeric Chain ◽  
Thermal Stabilities ◽  
Triethyl Amine ◽  
Ft Ir ◽  
Structure Confirmation

In this reserch Some new substituted and unsubstituted poly imides compounds. were synthesized by reaction of acrylol chloride with different amides (aliphatic and aromatic) in a suitable solvent in the presence amount triethyl amine (Et3N) with heating. The Structure confirmation of all polymers were confirmed using FT-IR,1H-NMR,13C-NMR and UV spectroscopy. Thermal analysis (TG) for some polymers showed their thermal stabilities. Other physical properties including softening points, melting point and solubility of the polymers were also measured

scholarly journals Lipase inhibitory activity assay for fermented milk

MethodsX ◽  
2020 ◽  
Vol 7 ◽  
pp. 100999
Author(s):  
Ana María Gil-Rodríguez ◽  
Thomas P. Beresford
Keyword(s):  
Inhibitory Activity ◽  
Fermented Milk ◽  
Activity Assay

The Synthesis, Characterization and Visible-Light Photodegradation Performance of Graphitic Carbon Nitride Coupling with CoAPO-5

2018 ◽  
Vol 281 ◽  
pp. 878-884
Author(s):  
Zhi Wei Zhou ◽  
Ling Fang Qiu ◽  
Xiao Bin Qiu ◽  
Shu Wang Duo
Keyword(s):  
Visible Light ◽  
Carbon Nitride ◽  
Diffuse Reflectance Spectroscopy ◽  
Light Illumination ◽  
X Ray Diffraction ◽  
Visible Absorption ◽  
X Ray ◽  
Grinding Method ◽  
Visible Light Illumination ◽  
Ft Ir

In order to enhance hole/electron separation and charge transfer in photocatalysts, the heterostructured g-C3N4/CoAPO-5 hybrids materials were synthesized via a simple grinding method and were investigated using X-ray diffraction (XRD), fourier transform infrared spectroscopy (FT-IR) and scanning electron microscopy (SEM). The optical properties of g-C3N4/CoAPO-5 hybrids materials were measured by ultraviolet-visible diffuse-reflectance spectroscopy (DRS), photoluminescence (PL) spectra and ultraviolet-visible absorption (UV-Vis) spectra. Under visible-light illumination, this work shows the heterogeneous g-C3N4/CoAPO-5 hybrids present a superior photocatalytic activity.

scholarly journals Synthesis and physical-chemical properties of some 5-(3-fluorophenyl)-4-methyl-1,2,4-triazole-3-thiol derivatives

2018 ◽  
pp. 38-47
Author(s):  
O. A. Bihdan ◽  
V. V. Parchenko
Keyword(s):  
Melting Point ◽  
Chemical Properties ◽  
Internal Standard ◽  
Automatic Device ◽  
Molecular Ions ◽  
Chemical Methods ◽  
Light Yellow ◽  
Physical Chemical ◽  
Methods Of Analysis ◽  
Complex Approach

There are engaged scientists practically from all over the world to the 1,2,4-triazole system research but the greatest attention deserve the achievements of domestic scientists who managed from the very beginning to register new original medicines in Ukraine. There is no doubt that the original attempt of combining various typical fragments with the nucleus of 1,2,4-triazole is gaining popularity among researchers. The purpose of our work was to synthesized and investigate a row of new 5-(3-fluorophenyl)-4-methyl-1,2,4-triazole-3-thiols by a Sulfur atom, to study the physical-chemical properties of previously unsubscribed compounds. The chemical names of the compounds are given in accordance with the IUPAC nomenclature (1979) and the IUPAC recommendations (1993). Investigations of the physical-chemical properties of the obtained compounds were carried out according to the methods which are given in the State Pharmacopoeia of Ukraine. The melting point was determined on an automatic device for determining the melting point OptiMelt Stanford Research Systems MPA100 (USA). The elemental structure of the new compounds was established on the element analyzer Elementar Vario L cube (CHNS) (standard - sulfanilamide). The data of elemental analysis correspond to the calculated. The 1Н NMR-spectra of the compounds were recorded using a «Mercury 400» spectrometer, the solvent DMSO-d6, the internal standard – tetramethylsilane (TMS) and decrypted using the SpinWorks computer program. Chromate-mass spectra were recorded on an Agilent 6890N/5973N/FID spectrometer produced by Agilent Technologies with a Dean microflow switch. By the experiment results there were obtained eleven previously unidentified individual compounds light yellow and white color which are soluble in organic solvents and insoluble in water. The crystallization process was carried out in isopropanol. Using a complex approach with the use of modern physical-chemical methods of analysis we confirmed the structure of 5-(3-fluorophenyl)-4-methyl-1,2,4-triazole-3-thiol, 3-alkylthio-5-(3-fluorophenyl)-4-methyl-1,2,4-triazole, 1,4-bis((5-(3-fluorophenyl)-4-methyl-1,2,4-triazole-3-yl)thio)propane and 1,4-bis((5-(3-fluorophenyl)-4-methyl-1,2,4-triazole-3-yl)thio)butane. The individuality of the synthesized compounds was confirmed chromatographically, the constants peaks of the pseudo molecular ions of the synthesized compounds coincide with the calculated values of the molecular masses. We first synthesized 5-(3-fluorophenyl)-4-methyl-1,2,4-triazol-3-thiol which was further used as a starting material in the synthesis of new 3-alkylthio-5-(3-fluorophenyl)-4-methyl-1,2,4-triazole, 1,4-bis((5-(3-fluorophenyl)-4-methyl-1,2,4-triazol-3-yl)thio)propane and 1,4-bis((5-(3-fluorophenyl)-4-methyl-1,2,4-triazol-3-yl)thio)butane. Complex physical-chemical methods of analysis confirmed the structure of synthesized compounds.

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