<i>N</i>-(4-((E)-3-Arylacryloyl)phenyl)acetamide Derivatives and their Antileishmanial Activity

Pacheco, Dency José; Trilleras, Jorge; Quiroga, Jairo; Gutierrez, J Millan; Prent-Peñaloza, Luis; Coavas, Tobinson; Marín, Juan Camilo; Delgado, Gabriela

doi:10.5935/0103-5053.20130203

Cited by 6 publications

(8 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…al., 2010), aumentando su importancia debido a la funcionalización de MWCNTs. Las bandas 1667 cm -1 y 1669 cm -1 describen la vibración del grupo C=C (Pacheco et al, 2013). Al analizar las bandas de 2493 cm -1 y 2521 cm -1 que corresponden al grupo C-O-H (Stobinski et.…”

Section: En La Figura 5 Se Muestran Las áReas Integradas Que Varían Cunclassified

Sintesis y Caracterización del Nanomaterial TiO2-MWCNTs (Oxido de Titanio-Nanotubos de Carbono de Pared Múltiple)

2016

View full text Add to dashboard Cite

ResumenEn este trabajo se estudió el efecto de agregar nanotubos de carbono de pared múltiple funcionalizados y sin funcionalizar durante la síntesis por sol-gel de TiO2 nanocerámico. La funcionalización de los nanotubos de carbono de pared múltiple se realizó mediante el método de carboxilación empleando HSO4-HNO3 y HCL. El precursor empleado para la fabricación del TiO2 fue Tetrabutóxido de Titanio, Ti(OBu)4. Las reacciones de hidrólisis y policondensación, el precalcinado y calcinado del proceso sol-gel, se siguieron y analizaron mediante Espectroscopia Infrarroja con Transformada Fourier (FTIR). Se obtuvieron nanocompuestos de TiO2 con proporciones de nanotubos de carbono de 0.0%, 0.7%, 1.4% y 2.1% en fracción másica. Por pruebas de nanoindentación y microindentación se determinó un aumento del 39% en dureza y la magnitud del módulo de Young aumentó dos veces. Con Microscopia Electrónica de Transmisión (TEM) se observaron detalles estructurales estableciendo homogeneidad y reducción en el tamaño de nanotubos de carbono. Palabras clave: nanotubos de carbono de pared múltiple; dióxido de titanio; funcionalización; proceso sol-gel Synthesis and Characterization of the Nanomaterial TiO2-MWCNTs (Titanium Oxide-Multi-Walled Carbon Nanotubes) AbstractThe effect of adding functionalized and non-functionalized multiwall carbon nanotubes to nano-ceramic material by the sol-gel process of nanoceramic TiO2 were studied. The functionalization of multiwall carbon nanotubes using the method of carboxylation with HSO4-HNO3 and HCl was developed. Tetrabuthoxide Titanium, Ti(OBu)4, was the precursor used for the manufacture of TiO2. The hydrolysis and polycondensation reactions, in addition to the pre-calcined and calcined in the sol-gel process were followed and analyzed by Fourier Transform Infrared Spectroscopy (FTIR). TiO2 with multiwall carbon nanotubes mass fraction of 0.0%, 0.7%, 1.4% and 2.1% were obtained. For nanoindentation and microindentación tests increase in hardness of 39% and increase of two times in the Young's modulus were observed. Structural details establishing uniformity and reduction in the size of multiwall carbon nanotubes were studied by Transmission Electron Microscopy (TEM).

show abstract

Section: En La Figura 5 Se Muestran Las áReas Integradas Que Varían Cunclassified

Sintesis y Caracterización del Nanomaterial TiO2-MWCNTs (Oxido de Titanio-Nanotubos de Carbono de Pared Múltiple)

2016

View full text Add to dashboard Cite

show abstract

“…[2][3][4][5][6] The acetamides are singled out from the rest of the derivatives of amides by the diversity of their pharmacological properties. It has been found that some derivatives of acetamides are used as antiprotozoics 7,8 , as bactericides 9 , in agriculture as insecticides 10 , herbicides 11 and fungicides. 12 It is not unknown that many of them are applied as analgesics 13 , anticonvulsants 14 and antioxidants.…”

Section: Introductionmentioning

confidence: 99%

Thin-Layer Chromatography on Reversed Phase in the Characterization of Retention Behaviour, Lipophilicity, and Pharmacokinetics of Cyanoacetamide Derivatives

Apostolov

Vastag

Matijević

et al. 2020

J. Chil. Chem. Soc.

View full text Add to dashboard Cite

Biological activity of a molecule is closely related to its lipophilicity. This significant parameter was determined for a group of potentially bioactive N-(4-phenylmonosubstituted)-2-cyanoacetamides applying thin-layer chromatography on reversed phase (RP-TLC) in mixtures of water and two organic modifiers separately, i-propanol and dioxane. The effect of the chemical structure of derivatives and the influence of the applied organic modifier on their retention were studied. The determined chromatographic retention constants, RM 0 , and the chromatographic parameter, m, of compounds were correlated with software calculated partition coefficients, log P as the standard measure of lipophilicity and with different pharmacokinetic predictors applying classical linear and multiple regression analysis. By classical linear regression analysis in both water-modifier systems only RM 0-log P and m-log P correlations were established (average r, 0.909 and 0.826). All studied relationships were enhanced by molecular descriptors that fulfilled the modified Lipinski's rule of five. Thereby, the performed multiple regression analysis gave better correlations (for RM 0-log P and m-log P average r 2 , 0.994 and 0.993; for RM 0-pharmacokinetic parameters and m-pharmacokinetic parameters average r 2 0.978 and 0.980). The obtained results indicate that the chromatographic parameters, RM 0 and m determined by RP-TLC at given conditions could be used successfully for the description of lipophilicity and the evaluation of pharmacokinetic properties of N-(4-phenylmonosubstituted)-2-cyanoacetamides as potential bioactive molecules.

show abstract

“…Moreover, recently particular attention was given to numerous derivatives of acetamides by the researchers as these molecules exhibit different biological activity such as antibacterial and antifungal (Ertan et al, 2007, Jamkhandi and Disouza, 2012, Hamad et al, 2017, antiinflammatory (de Castro Barbosa et al, 2009), antilieshmania (Pacheco et al, 2013), antituberculosis (Yadav et al, 2018), insecticide (Kalyanasundaram and Mathew, 2006), anthelmintic (Sawant and Kawade, 2011), antioxidant and anticancer (Özkay et al, 2010, Chen et al, 2013, Pawar et al, 2017, anticonvulsant and antidepressant (Soyer et al, 2004, Tarikogullari et al, 2010, Guan et al, 2016. In this study, various NSAIDs 2a-f were attached to N-(2,6-dimethyl phenyl) acetamide 1 to decrease the gastric irritation by masking the acidic carboxylic group through ester linkage as shown in Scheme 1.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization, and Antibacterial Activity of Novel Mutual Non-Steroidal Anti-inflammatory Prodrugs

hamadameen

Ameen

2019

ZJPAS

View full text Add to dashboard Cite

Non steroidal anti-inflammatory drugs (NSAIDs) are among the most used analgesic and anti-inflammatory drugs. However inhibition of cyclooxygenase1 and acidic groups such as carboxylic groups in most NSAIDs cause gastrointestinal (GI) side effects. Therefore masking the acidic groups till it pass through the GI tract will decrease the direct GI side effects and because N-(2,6-dimethylphenyl)-acetamide 1 also has anti-inflammatory activity so the synthesized ester prodrugs might act as mutual prodrugs. Moreover, because of emerging of new strains of bacteria and resistance of bacteria to the available antibacterial agents, new antibacterial agents are needed. The NSAIDs have antibacterial activity and N-(2,6-dimethylphenyl) acetamide 1 also has antibacterial activity so binding of these molecules with each other might give more potent antibacterial agent. 2-Chloro-N-(2,6dimethyl phenyl) acetamide 1 was utilized to synthesize ester prodrug of various NSAIDs 2a-f. The 2-Chloro-N-(2,6dimethylphenyl)-acetamide 1 undergo substitution reaction at α position with various sodium carboxylate of NSAIDs 2a-f in DMSO. The constitution of the newly synthesized ester prodrugs of NSAIDs 3a-f had been confirmed on the basis of their IR, ¹H and ¹³C-NMR spectral data. All the synthesized ester prodrugs 3a-f were screened for their in vitro antibacterial activities against Staphylococcus aureus ATCC 25923 and Escherichia coli ATCC 25922 however, their antibacterial activity decreased compared with their starting 1 and 2a-f.

show abstract

N-(4-((E)-3-Arylacryloyl)phenyl)acetamide Derivatives and their Antileishmanial Activity

Cited by 6 publications

References 0 publications

Sintesis y Caracterización del Nanomaterial TiO2-MWCNTs (Oxido de Titanio-Nanotubos de Carbono de Pared Múltiple)

Sintesis y Caracterización del Nanomaterial TiO2-MWCNTs (Oxido de Titanio-Nanotubos de Carbono de Pared Múltiple)

Thin-Layer Chromatography on Reversed Phase in the Characterization of Retention Behaviour, Lipophilicity, and Pharmacokinetics of Cyanoacetamide Derivatives

Synthesis, Characterization, and Antibacterial Activity of Novel Mutual Non-Steroidal Anti-inflammatory Prodrugs

Contact Info

Product

Resources

About