MANIFESTATION OF THE gauche EFFECT IN CONFORMERS OF BENZENESULFONIC ACID HYDRAZIDE

2017 ◽  
Keyword(s):  
Acid Hydrazide ◽  
Benzenesulfonic Acid ◽  
Gauche Effect

Synthesis of Some New Tetracyclic Pyrimidine Derivatives Using Exocyclic α,β-Unsaturated Ketone and Evaluation of Their Antitumor Activities

2016 ◽  
Vol 12 (8) ◽  
pp. 311-317
Author(s):  
Kamelia El-Mahdy
Keyword(s):  
Antitumor Activity ◽  
Spectroscopic Data ◽  
Acid Hydrazide ◽  
Chloroacetic Acid ◽  
Equimolar Amount ◽  
Unsaturated Ketone ◽  
Cyanoacetic Acid ◽  
Antitumor Activities ◽  
Pyrimidine Derivatives ◽  
Cyanoacetic Acid Hydrazide

Thiazolopyrimidine 2 was obtained from the reaction of dihydropyrimidinone with chloroacetic acid and benzaldehyde. Thiazolopyrimidine 2 containing an α,β-unsaturated ketonic function [-CH=CH-CO-] has been used as a component of Michael addition with an equimolar amount of dinucleophiles to give a series of novel tetracyclic pyrimidine derivatives. Treatment of thiazolopyrimidine 2 with uracil, aminotriazole, cyanoacetic acid hydrazide, o-phenylenediamine or diaminopyridine afforded the corresponding pyridopyrimidine, triazolopyrimidine, pyrazolone, benzodiazepine and triazepine derivative, respectively. The detailed synthesis, spectroscopic data, and antitumor activity for synthesized compounds were reported.

Hybrid Design of Isonicotinic Acid Hydrazide Derivatives: Machine Learning Studies, Synthesis and Biological Evaluation of their Antituberculosis Activity

2020 ◽  
Vol 17 (3) ◽  
pp. 365-375
Author(s):  
Vasyl Kovalishyn ◽  
Diana Hodyna ◽  
Vitaliy O. Sinenko ◽  
Volodymyr Blagodatny ◽  
Ivan Semenyuta ◽  
...  
Keyword(s):  
Machine Learning ◽  
Isonicotinic Acid ◽  
Acid Hydrazide ◽  
Predictive Ability ◽  
Antitubercular Activity ◽  
Biological Evaluation ◽  
Starting Point ◽  
Binary Classifiers ◽  
Synthesis And Biological Evaluation

Background: Tuberculosis (TB) is an infection disease caused by Mycobacterium tuberculosis (Mtb) bacteria. One of the main causes of mortality from TB is the problem of Mtb resistance to known drugs. Objective: The goal of this work is to identify potent small molecule anti-TB agents by machine learning, synthesis and biological evaluation. Methods: The On-line Chemical Database and Modeling Environment (OCHEM) was used to build predictive machine learning models. Seven compounds were synthesized and tested in vitro for their antitubercular activity against H37Rv and resistant Mtb strains. Results: A set of predictive models was built with OCHEM based on a set of previously synthesized isoniazid (INH) derivatives containing a thiazole core and tested against Mtb. The predictive ability of the models was tested by a 5-fold cross-validation, and resulted in balanced accuracies (BA) of 61–78% for the binary classifiers. Test set validation showed that the models could be instrumental in predicting anti- TB activity with a reasonable accuracy (with BA = 67–79 %) within the applicability domain. Seven designed compounds were synthesized and demonstrated activity against both the H37Rv and multidrugresistant (MDR) Mtb strains resistant to rifampicin and isoniazid. According to the acute toxicity evaluation in Daphnia magna neonates, six compounds were classified as moderately toxic (LD50 in the range of 10−100 mg/L) and one as practically harmless (LD50 in the range of 100−1000 mg/L). Conclusion: The newly identified compounds may represent a starting point for further development of therapies against Mtb. The developed models are available online at OCHEM http://ochem.eu/article/11 1066 and can be used to virtually screen for potential compounds with anti-TB activity.

Synthesis and solvatochromic studies of 2- amino-3-phenolazo1-(4-sulfophenyl)-3-methyi-5-pyrozolone and use it for the determination of trace amount of Nickel (II) in blood samples

2016 ◽  
Vol 5 (10) ◽  
pp. 4920
Author(s):  
Amar M. Ali ◽  
Hussain. J. Mohammed*
Keyword(s):  
Stability Constant ◽  
Trace Amount ◽  
Benzenesulfonic Acid ◽  
Determination Method ◽  
Blood Samples ◽  
Determination Of Nickel ◽  
Normal Human ◽  
The Stability ◽  
Normal Human Blood

A new, simple, sensitive and rapid spectrophotometric method is proposed for the determination of trace amount of Nickel (II). The method is based on the formation of a 1:2 complex with 4-(4-((2-hydroxy-6-nitrophenyl) diazenyl) -3-methyl-5-oxo-2, 5-dihydro-1H-pyrazol-1-yl) benzenesulfonic acid (2-ANASP) as a new reagent is developed. The complex has a maximum absorption at 516 nm and εmax of 1. 84 X 105 L. mol-1. cm-1. A linear correlation (0. 25 – 4. 0μg. ml-1) was found between absorbance at λmax and concentration. The accuracy and reproducibility of the determination method for various known amounts of Nickel (II) were tested. The results obtained are both precise (RSD was 1. 2 %) and accurate (relative error was 0. 787 %). The effect of diverse ions on the determination of Nickel (II) to investigate the selectivity of the method were also studied. The stability constant of the product was 0. 399 X 106 L. mol-1. The proposed method was successfully applied to the analysis of diabetes blood and normal human blood. 

Benzenesulfonic acid-based hydrotropic system for achieving lignocellulose separation and utilization under mild conditions

2021 ◽  
pp. 125379
Author(s):  
Maolin Dong ◽  
Chen Wu ◽  
Lidong Chen ◽  
Xuelian Zhou ◽  
Weisheng Yang ◽  
...  
Keyword(s):  
Benzenesulfonic Acid ◽  
Mild Conditions

Mechanism of Bifunctional p-amino Benzenesulfonic Acid Modified Interface in Perovskite Solar Cells

2021 ◽  
pp. 129579
Author(s):  
Yapeng Sun ◽  
Jiankai Zhang ◽  
Huangzhong Yu ◽  
Jianming Wang ◽  
Chengwen Huang ◽  
...  
Keyword(s):  
Solar Cells ◽  
Perovskite Solar Cells ◽  
Benzenesulfonic Acid

scholarly journals THE ISOLATION AND PROPERTIES OF THE ISONICOTINIC ACID HYDRAZIDE ANALOGUE OF DIPHOSPHOPYRIDINE NUCLEOTIDE

1954 ◽  
Vol 209 (2) ◽  
pp. 467-484 ◽  
Author(s):  
Leonard J. Zatman ◽  
Nathan O. Kaplan ◽  
Sidney P. Colowick ◽  
Margaret M. Ciotti
Keyword(s):  
Isonicotinic Acid ◽  
Acid Hydrazide ◽  
Isonicotinic Acid Hydrazide
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