Oxidation of cyclic N-(arylamino)imides. An EPR study of hydrazoxyl radicals

1988 ◽  
Vol 53 (2) ◽  
pp. 243-250 ◽  
Author(s):  
Ladislav Omelka ◽  
Michael Reinhardt ◽  
Ralph Kluge ◽  
Manfred Schulz
Keyword(s):  
Spectroscopic Method ◽  
Phenyl Group ◽  
Spectral Simulation ◽  
Effect Of Substituents ◽  
Hammett Constants

New types of hydrazoxyl radicals were identified by ESR spectroscopic method during oxidation of N-(arylamino)imides. The ESR parameters of radicals generated were obtained by a spectral simulation. The effect of substituents on the values of splitting constants of nitrogen atoms N1 and N2 is discussed. The splitting constants a(N1) well correlate with the σ-Hammett constants of substituents of the 1-phenyl group.

Quantitative relations between chemical structure and hepatotoxicity of thiobenzamides

1988 ◽  
Vol 53 (11) ◽  
pp. 2957-2961 ◽  
Author(s):  
Karel Waisser ◽  
Miloš Macháček ◽  
Jean Lebvoua ◽  
Jiří Hrbata ◽  
Jaroslav Dršata
Keyword(s):  
Chemical Structure ◽  
Chemical Shifts ◽  
Phenyl Group ◽  
Total Effect ◽  
Nmr Chemical Shifts ◽  
H Nmr ◽  
Hammett Constants ◽  
Thioamide Group

1H NMR chemical shifts of thioamide protons have been determined for a group of thiobenzamides, and the values obtained have been correlated with the Hammett constants. From the relations found the σm and σp values of thioamide group and some other σ constants describing the total effect of two substituents in the phenyl group have been calculated. The relation between the hepatotoxicity for rats (expressed as log ALT) and the Hammett constants is described by equation of parabola.

Synthesis and insecticidal activity of lipophilic amides. Part 4: The effect of substituents on the phenyl group of 6-phenylhexa-2,4-dienamides

1987 ◽  
Vol 18 (4) ◽  
pp. 223-228 ◽  
Author(s):  
Michael Elliott ◽  
Andrew W. Farnham ◽  
Norman F. Janes ◽  
Diana M. Johnson ◽  
David A. Pulman
Keyword(s):  
Insecticidal Activity ◽  
Phenyl Group ◽  
Effect Of Substituents

Substituent effects in the reaction of aromatic amines and peroxydisulfate

1969 ◽  
Vol 47 (19) ◽  
pp. 3710-3713 ◽  
Author(s):  
N. Venkatasubramanian ◽  
A. Sabesan
Keyword(s):  
Nitrogen Atom ◽  
Carbon Atom ◽  
Aromatic Amines ◽  
Substituent Effects ◽  
Substituted Anilines ◽  
Electrophilic Attack ◽  
Effect Of Substituents ◽  
Hammett Constants ◽  
Kinetics Of ◽  
Electron Withdrawing Substituents

The kinetics of the reaction between aromatic amines and the peroxydisulfate ion in aqueous basic conditions have been investigated. The effect of substituents has been studied by employing about 25 ortho-, meta-, and para-substituted anilines. The reaction is accelerated by electron-releasing substituents and is retarded by electron-withdrawing substituents, pointing to an electrophilic attack by the S2O82− ion. A better correlation between rate and the Hammett constants is obtained for an electrophilic attack at the nitrogen atom of the amine rather than at the carbon atom of the amine. A good correlation also exists between the log k2 values and the pKb of the corresponding amines.

Laser-induced switching of the biological activity of phosphonate molecules

2021 ◽  
Author(s):  
Ilya Kolesnikov ◽  
Anastasia Khokhlova ◽  
Dmitrii Pankin ◽  
Anna Pilip ◽  
Anastasia Egorova ◽  
...  
Keyword(s):  
Biological Activity ◽  
Laser Irradiation ◽  
Phenyl Group ◽  
Effect Of Substituents ◽  
First Time ◽  
Butyrylcholinesterase Inhibition

Butyrylcholinesterase inhibition and its enhancement as a result of laser irradiation are demonstrated for the first time for a series of phosphorylated arylaminomalonates. Effect of substituents in phenyl group on...

Effect of substituents at phenyl group of 7,7′-dioxo-9,9′-epoxylignane on antifungal activity

2012 ◽  
Vol 22 (21) ◽  
pp. 6740-6744 ◽  
Author(s):  
Hisashi Nishiwaki ◽  
Maya Ouchi ◽  
Junko Matsugi ◽  
Koichi Akiyama ◽  
Takuya Sugahara ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Phenyl Group ◽  
Effect Of Substituents

UV spectroscopic method for determination of phenytoin in bulk and injection forms

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Quality Control ◽  
Spectrophotometric Method ◽  
Spectroscopic Method ◽  
Ich Guidelines ◽  
Precision And Accuracy ◽  
Routine Quality Control

Recent study was conducted to develop a simple UV spectrophotometric method to determine Phenytoin in bulk and injection form according to official requirement and validate as per ICH guidelines. λmax of Phenytoin was found 202 nm. Linearity existed perceived in the concentration assortment 2-8 μg/ml (r2 = 0.999) for the method. The method was validated pertaining to linearity, precision and accuracy studies, LOD and LOQ consistent with ICH guidelines. The existent method was establish to be simple, linear, precise, accurate as well as sensitive and can be applied for routine quality control enquiry for the analysis of Phenytoin in bulk and injection form.

Development and Validation of Derivative Spectroscopic Method for Simultaneous Estimation of Cefadroxil and Probenecid

2014 ◽  
Vol 7 (1) ◽  
pp. 2350-2355
Author(s):  
Pratik S Mehta ◽  
Pratik R. Patel ◽  
Rajesh R Parmar ◽  
M M K Modasiya ◽  
Dushyant A Shah
Keyword(s):  
Spectroscopic Method ◽  
Spectral Interference ◽  
Synthetic Mixture ◽  
Simultaneous Estimation ◽  
Zero Crossing ◽  
First Order ◽  
Derivative Spectroscopy ◽  
Development And Validation ◽  
Crossing Point

A novel, simple, accurate, sensitive, precise and economical derivative spectroscopic method was developed and validated for the determination of cefadroxil and probenecid in synthetic mixture. First order derivative spectroscopy method was adopted to eliminate spectral interference. The method obeys Beer’s Law in concentration ranges of 4-36 μg/ml for cefadroxil and of 5-25 μg/ml of probenecid. The zero crossing point for cefadroxil and probenecid was 260 nm and 237.8 nm respectively in 0.1N HCl. The method was validated in terms of accuracy, precision, linearity, limits of detection, limits of quantitation. This method has been successively applied to synthetic mixture and no interference from the synthetic mixture’s excipients was found.   

4-Aryl-1,4-Dihydropyridines as Potential Enoyl-Acyl Carrier Protein Reductase Inhibitors: Antitubercular Activity and Molecular Docking Study

2020 ◽  
Vol 20 ◽  
Author(s):  
Katharigatta N. Venugopala ◽  
Christophe Tratrat ◽  
Melendhran Pillay ◽  
Pran Kishore Deb ◽  
Deepak Chopra ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Acyl Carrier Protein ◽  
Phenyl Group ◽  
Antitubercular Activity ◽  
Docking Study ◽  
Benzyl Ester ◽  
Multi Drug Resistance ◽  
Carrier Protein ◽  
Molecular Docking Study ◽  
Lipinski’S Rule

Background: Tuberculosis remains one of the most deadly infectious diseases worldwide due to the emergence of multi-drug resistance (MDR) and extensively drug resistance (XDR) strains of Mycobacterium tuberculosis (MTB). Materials and Methods: Herein, the screening of a total of eight symmetrical 1,4-dihydropyridine (1,4-DHP) derivatives (4a-4h) was carried out for whole-cell anti-TB activity against the susceptible H37Rv and MDR strains of MTB. Results and Discussion: Most of the compounds exhibited moderate to excellent activity against the susceptible H37Rv. Moreover, the most promising compound 4f (against H37Rv) having para-trifluoromethyl phenyl group at 4-position and bis para-methoxy benzyl ester group at 3- and 5-positions of 1,4-dihydropyridine pharmacophore, exhibited no toxicity, but demonstrated weak activity against MTB strains resistant to isoniazid and rifampicin. In light of the inhibitory profile of the title compounds, enoyl-acyl carrier protein reductase (InhA) appeared to be the appropriate molecular target. Docking study of these derivatives against InhA receptor revealed favorable binding interactions. Further, in silico predicted ADME properties of these compounds 4a-4h were found to be in the acceptable ranges including satisfactory Lipinski’s rule of five, thereby indicating their potential as drug-like molecules. Conclusion: In particular, the 1,4-DHP derivative 4f can be considered as an attractive lead molecule for further exploration and development of more potent anti-TB agents as InhA inhibitors.

Screening of Actinomycetes For α-amylase Inhibitors Production

2019 ◽  
Vol 15 (1) ◽  
pp. 41-45
Author(s):  
Shivabai Chandwad ◽  
Sudhakar Gutte
Keyword(s):  
Inhibitory Activity ◽  
Enzyme Inhibitors ◽  
Spectroscopic Method ◽  
Solid Material ◽  
Soil Samples ◽  
Assay Method ◽  
Novel Drugs ◽  
Pre Treatment ◽  
Diabetic Treatment ◽  
Amylase Inhibitors

Background:Diabetes mellitus is the most common and fastest growing disease in the world. One of the therapies to treat diabetes is the inhibition of α-amylase activity by inhibitors from microbial and plant source. Actinomycetes are potential sources of enzyme inhibitors, drugs, amino acids, vitamins etc.Objective:Our work mainly highlights the isolation of actinomycetes from soil samples of different habitats and screening of α -amylase inhibitors.Methods:Actinomycetes were isolated from soil samples of different habitats by different methods; these include a variety of pre-treatment of soil samples in combination with an appropriate supplement medium with selective antibacterial agents. Isolated actinomycetes grown in fermentation condition and metabolites were extracted with Isopropyl alcohol and concentrated to obtain solid material. The extract of each isolate was tested for α -amylase inhibition using starch Iodine plate method and DNS- spectroscopic method.Results:Total 110 actinomycetes strains were isolated from various sources. Among 110 extracts of actinomycetes, eight extracts have shown positive results for α-amylase inhibition in starch Iodine plate assay method. Extracts selected from primary results were used for the confirmation of inhibitory activity using DNS- spectroscopic method. Out of eight extracts, six extracts showed Porcine pancreatic α -amylase inhibitory activity ranging from 40-86%. The actinomycetes strains that produce α -amylase inhibitory activity are A-24, A-29, B-5, B-18, C-15 and D-24.Conclusion:These results show that actinomycetes are a potential source for α -amylase inhibitors, which may lead to valuable novel drugs for diabetic treatment.

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