Synthesis and Biological Activity of N-(arylsulfonyl) Valine Hydrazones and Assistance of NMR Spectroscopy for Definitive 3D Structure

2019 ◽  
Vol 16 (9) ◽  
pp. 974-983 ◽  
Author(s):  
Sevil Şenkardeş ◽  
Esra Tatar ◽  
Ridvan Nepravishta ◽  
Dorisa Cela ◽  
Maurizio Paci ◽  
...  
Keyword(s):  
3D Structure ◽  
Acid Hydrazide ◽  
Biologically Active ◽  
Myelogenous Leukemia ◽  
Side Chain ◽  
Amino Acid Side Chain ◽  
Ic50 Values ◽  
Compound 21

Background:Hydrazide-hydrazones constitute an important class of compounds for new drug development. In this study, a series of 39 new acylhydrazones (3-41), derived from (2S)-3-methyl- 2-[[(4-methylphenyl)sulfonyl]amino]butanoic acid hydrazide were synthesized with further aim to achieve biologically active acylhydrazones carrying an amino acid side chain.Methods:Compounds 3-41 were synthesized by microwave-assisted method. All synthesized compounds have been tested for their anti-HIV activity compound 21 was subjected to a new set of 2DNMR analysis for the characterization of the isomers in solution and determination of its 3D structure.Results:The IC50 values for compounds 2-40 were found between >125-10.90 µg/ml against HIV- 1(IIIB) and HIV-2(ROD) strains in MT-4 cells. Compounds 3, 6, 10, 12, 23, 24, 27, 32, and 37 with CC50 values between 10.90-14.50 µg/ml were selected to evaluate for their antileukemia activity. IC50 values for these mentioned compounds were found as >100μM on human chronic myelogenous leukemia, K562 cell line.Conclusion:Some compounds with IC50 values between 10.90-14.50 μg/ml will be of benefit in the development of novel leads.

scholarly journals Characterization of Hapten-Protein Conjugates: Antibody Generation and Immunoassay Development for Chlorophenoxyacetic Acid Pesticides

2009 ◽  
Vol 92 (6) ◽  
pp. 1773-1779 ◽  
Author(s):  
Robin C Boro ◽  
K Vikas Singh ◽  
C Raman Suri
Keyword(s):  
Inhibitory Concentration ◽  
Dichlorophenoxyacetic Acid ◽  
Protein Conjugation ◽  
Protein Conjugates ◽  
Highly Sensitive ◽  
Ic50 Values ◽  
Chlorophenoxyacetic Acid ◽  
2,4 Dichlorophenoxyacetic Acid

Abstract The generation of specific and sensitive antibodies against small molecules is greatly dependent upon the characteristics of the hapten-protein conjugates. In this study, we report a new fluorescence-based method for the characterization of hapten-protein conjugates. The method is based on an effect promoted by hapten-protein conjugation density upon the fluorescence intensity of the intrinsic tryptophan chromophore molecules of the protein. The proposed methodology is applied to quantify the hapten-protein conjugation density for two different chlorophenoxyacetic acid pesticides, 2,4-dichlorophenoxyacetic acid (2,4-D) and 2,4-dichlorophenoxybutyric acid (2,4-DB), coupled to carrier protein. Highly sensitive anti-2,4-D and anti-2,4-DB antibodies were obtained using these well-characterized hapten-protein conjugates. The generated antibodies were used in an immunoassay format demonstrating inhibitory concentration (IC50) values equal to 30 and 7 ng/mL for 2,4-D and 2,4-DB, respectively. Linearity was observed in the concentration range between 0.1500 ng/mL with LODs around 4 and 3 ng/mL for 2,4-D and 2,4-DB, respectively, in standard water samples. The proposed method was successfully applied for the determination of the extent of hapten-protein conjugation to produce specific antibodies for immunoassay development against pesticides.

scholarly journals Voltammetric Characterization of the Behavior of Biologically Active Compound Enoxil in Various Media

2011 ◽  
Vol 6 (1) ◽  
pp. 62-68
Author(s):  
Gheorghe Nemţoi ◽  
Tudor Lupaşcu ◽  
Alexandra Ciomaga ◽  
Alexandru Cecal
Keyword(s):  
Sodium Perchlorate ◽  
Reduction Process ◽  
Oxidation Potential ◽  
Biologically Active ◽  
Aqueous Environment ◽  
Cathodic Current ◽  
Oxidation Reduction ◽  
Complex Preparation

This paper presents the results of scientific research related to the electrochemical behavior of the complex preparation Enoxil. It was established that the oxidation-reduction process of Enoxil is quasireversible. The reactivity of Enoxil obtained from alcohol soluble enotannins is more pronounced, compared to that obtained from standard enotannins. The dependence of cathodic current intensity on Enoxil concentration is linear. This can be used to establish Enoxil concentration in solution. Cyclic voltamograms were used to establish reduction and oxidation potential and the formal redox potential on platinum electrode in sodium perchlorate aqueous environment. These features can be used for identification and determination of Enoxil in pharmaceuticals.

Untersuchungen an biologisch wirksamen Ligandensystemen, XII1 Metallkomplexe des Maleinsäurehydrazids und ihre physiologische Wirkung auf Yoshida-Sarkom-Asciteszellen / Investigations of Biologically Active Ligands, XII1 Metal Complexes of Maleic Acid Hydrazide and their Physiologic Action on Yoshida-Sarcoma Ascites Cells

1977 ◽  
Vol 32 (4) ◽  
pp. 393-400 ◽  
Author(s):  
Heinz P. Fritz ◽  
Bernhard Lippert ◽  
Kurt Possinger ◽  
Reiner Hartenstein
Keyword(s):  
Metal Complexes ◽  
Maleic Acid ◽  
Acid Hydrazide ◽  
Biologically Active ◽  
Yoshida Sarcoma ◽  
Pt Complex

The preparation and characterization of metal complexes of maleic acid hydrazide is reported, including Ca, Mn, Fe, Co, Ni, Cu, Zn and Pt-complexes, as well as the action of maleic acid hydrazide and one Pt-complex on Yoshida-ascites-sarcoma.

Characterization of 10 Biogenic Amines in Male Silkworm Moth by HPLC with Precolumn Derivatization

2020 ◽  
Vol 16 (5) ◽  
pp. 608-614
Author(s):  
Mingqin Fan ◽  
Yun Ai ◽  
Wenjie Zhao ◽  
Yanni Sun ◽  
Jianli Liu ◽  
...  
Keyword(s):  
Biogenic Amines ◽  
Biologically Active ◽  
Low Molecular Weight ◽  
Precolumn Derivatization ◽  
Mean Values ◽  
The Mean ◽  
Toxic Potential ◽  
First Time

Background: Biogenic Amines (BAs) are biologically active nitrogenous organic compounds of low molecular weight, which are frequently found in a wide variety of foods, beverages and herbs due to their toxic potential in humans. Male Silkworm Moth (MSM), a Traditional Chinese Medicine (TCM), has been exploited and utilized as nutritious liquor based on its traditional effects in the Chinese community. Objective: The objective of this study was to develop an HPLC with Dns-Cl derivatization method for characterizing overall BAs in MSM and providing data for further evaluating its activities and safety profiles. Methods: The method has acceptable sensitivity, precision, accuracy, selectivity and recovery, and was successfully applied to the determination of the BAs contents in MSM for the first time. Results: In the analysis of 10 batches of MSM samples, serotonin and dopamine were not found in detectable concentrations in any samples, and the most abundant amine found was putrescine. The mean values of tryptamine, phenylethylamine, putrescine, cadaverine, histamine, tyramine, spermidine, and spermine determined in the samples were found to be 34.7 mg/ kg, 16.1 mg/ kg, 218.3 mg/ kg, 37.9 mg/ kg, 12.1 mg/ kg, 18.2 mg/ kg, 4.5mg/ kg, and 0.9 mg/ kg, respectively. Conclusion: The contents of BAs in 10 batches of MSM were below the maximum recommended limits, and MSM can be used safely.

scholarly journals An Integrated Characterization of Jujube (Ziziphus jujuba Mill.) Grown in the North Adriatic Region

2019 ◽  
Vol 57 (1) ◽  
pp. 17-28
Author(s):  
Ana Miklavčič Višnjevec ◽  
Ajda Ota ◽  
Dunja Bandelj ◽  
Nataša Poklar Ulrih ◽  
Milena Bučar-Miklavčič ◽  
...  
Keyword(s):  
Phenolic Compounds ◽  
Positive Impact ◽  
Dry Mass ◽  
Biologically Active ◽  
Aqueous Extracts ◽  
Local Variety ◽  
Jujube Fruit ◽  
Ziziphus Jujuba

Jujube (Ziziphus jujuba Mill.) has favourable horticultural properties including adaptation to arid conditions, abiotic and biotic stresses, as well as positive impact on human health. The present study describes the characterization of genetic diversity of the germ­plasm of jujube from the Istrian peninsula, the determination of important chemical compounds, antioxidative properties in relation to antibacterial and antifungal activities of jujube fruit extracts, and the determination of nutritional properties of jujube fruit. The results of the genetic analysis showed that most of the samples from the Istrian peninsula belong to two recently introduced varieties, 'Li' and 'Lang', and the most widespread local variety 'Navadna žižola'. The local variety has smaller fruit than the ‘Li’ and ‘Lang’ varieties, with thick and fleshy mesocarp. Chemical analysis indicated that fruits of the local variety contained a valuable source of dietary fibre ((9.7±0.6) g/100 g) and were rich in minerals such as (in g/100 g dry mass): potassium (829±51), calcium (177±11) and phosphorus (129±19). Aqueous extracts showed slight antibacterial activity, while ethanol extracts had higher mass fractions of phenolic compounds (expressed as gallic acid equivalents (GAE), 5.8-8.7 mg/g) than the aqueous extracts, but did not show antimicrobial activity. Compounds other than phenolic compounds in jujube fruit may be more biologically active. Based on the results of these analyses, the local Istrian jujube variety is a promising candidate for cultivation potential.

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