scholarly journals Binary Mixtures of (N-phosphonomethyl)-glycine with New Aminophosphonates

2004 ◽  
Vol 59 (7-8) ◽  
pp. 515-518 ◽  
Author(s):  
Krzysztof Bielecki ◽  
Janusz Sarapuk ◽  
Halina Kleszczynáska
Keyword(s):  
Biological Activity ◽  
Binary Mixtures ◽  
Structural Features ◽  
Wheat Growth ◽  
Inhibition Of Growth ◽  
Additive Type ◽  
Order Of Magnitude ◽  
Organophosphorous Compounds ◽  
New Compounds ◽  
Potential Use

AbstractThe potential biological activity of binary mixtures of some new organophosphorous compounds, aminoalkane- and aminofluorenephosphonates, with (N-phosphonomethyl)-glycine (glyphosate, PMG) was studied. The inhibition of growth of wheat (Triticum aestivum) induced by individual compounds and their equimolar mixtures with PMG was a measure of that activity. The experiments were expected to show if the new compounds exhibited good biological activity to be used for agrochemical applications and if this activity can be improved when they are used in mixtures with glyphosate which is the active component of the well-known herbicide Roundup. The results obtained show that aminofluorenephosphonates inhibited wheat growth when used in micromolar concentrations. Thus, their efficiency can be compared to that of PMG. The efficiency of aminoalkanephosphonates was one order of magnitude weaker. The measure of the efficiency was the effective concentration inhibiting wheat growth by 50% (EC50). The most demanded interaction, i.e., a synergistic was observed for only one of binary mixtures of the compounds studied with PMG. Mostly they showed antagonistic or strong antagonistic interactions. Some of them were of the additive type. Such results exclude the possibility of potential use of all the compounds studied in binary mixtures with phosphonomethylglycine, especially as the mentioned synergistic interaction found was rather weak. The influence of structural features of aminophosphonates on the results obtained is discussed.

scholarly journals MODERN ETHIOTROPIC CHEMOTHERAPY OF HERPESVIRUS INFECTIONS: ADVANCES, NEW TRENDS AND PERSPECTIVES. ALPHAHERPESVIRINAE (part I)

2018 ◽  
Vol 63 (3) ◽  
pp. 106-114
Author(s):  
V. L. Andronova
Keyword(s):  
Drug Resistance ◽  
Biological Activity ◽  
Dna Polymerase ◽  
Antiviral Agents ◽  
Structural Features ◽  
Modern Medicine ◽  
Antiviral Drugs ◽  
Modified Nucleosides ◽  
Herpesvirus Infection ◽  
New Compounds

Modern therapy of infections caused by alpha-herpesviruses is based on drugs belonging to the class of modified nucleosides (acyclovir) and their metabolic progenitors - valine ester of acyclovir and famciclovir (prodrug of penciclovir). The biological activity of these compounds is determined by the similarity of their structure to natural nucleosides: modified nucleosides compete with natural nucleosides for binding to DNA-polymerase and, due to their structural features, inhibit its activity. However, the emergence of variants of viruses resistant to the antiviral drugs available in the arsenal of modern medicine necessitates the search for new compounds able of effectively inhibiting the reproduction of viruses. These compounds should be harmless to the macroorganisms, convenient to use, and overcoming the drug resistance barrier in viruses. The search for literature in international databases (PubMed, MedLine, RINC, etc.) in order to obtain information on promising developments that open new possibilities for treating herpesvirus infection and subsequent analysis of the collected data made it possible to determine not only the main trends in the search for new antiviral agents, but also to provide information on the compounds most promising for the development of anti-herpesvirus drugs.

scholarly journals Metabolomic Study of Heterotrophically Grown Chlorella sp. Isolated from Wastewater in Northern Sweden

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2410
Author(s):  
Jean Claude Nzayisenga ◽  
Anita Sellstedt
Keyword(s):  
Sustainable Development ◽  
Butyric Acid ◽  
Lipid Production ◽  
Growth Conditions ◽  
Northern Sweden ◽  
Metabolic Intermediate ◽  
Chlorella Sp ◽  
Lipid Contents ◽  
New Compounds ◽  
Potential Use

There are numerous strains of Chlorella with a corresponding variety of metabolic pathways. A strain we previously isolated from wastewater in northern Sweden can grow heterotrophically as well as autotrophically in light and has higher lipid contents under heterotrophic growth conditions. The aims of the present study were to characterize metabolic changes associated with the higher lipid contents in order to enhance our understanding of lipid production in microalgae and potentially identify new compounds with utility in sustainable development. Inter alia, the amino acids glutamine and lysine were 7-fold more abundant under heterotrophic conditions, the key metabolic intermediate alpha-ketoglutarate was more abundant under heterotrophic conditions with glucose, and maltose was more abundant under heterotrophic conditions with glycerol than under autotrophic conditions. The metabolite 3-hydroxy-butyric acid, the direct precursor of the biodegradable plastic PHB (poly-3-hydroxy-butyric acid), was also more abundant under heterotrophic conditions. Our metabolomic analysis has provided new insights into the alga’s lipid production pathways and identified metabolites with potential use in sustainable development, such as the production of renewable, biodegradable plastics, cosmetics, and nutraceuticals, with reduced pollution and improvements in both ecological and human health.

scholarly journals Development of Antibacterial and Antifungal Triazole Chromium(III) and Cobalt(II) Complexes: Synthesis and Biological Activity Evaluations

Molecules ◽  
2018 ◽  
Vol 23 (8) ◽  
pp. 2013 ◽  
Author(s):  
Ricardo Murcia ◽  
Sandra Leal ◽  
Martha Roa ◽  
Edgar Nagles ◽  
Alvaro Muñoz-Castro ◽  
...  
Keyword(s):  
Electrical Conductivity ◽  
Biological Activity ◽  
Melting Point ◽  
Inhibitory Concentration ◽  
Vero Cells ◽  
Visible Spectroscopy ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal ◽  
New Compounds

In this work, six complexes (2–7) of Cr(III) and Co(II) transition metals with triazole ligands were synthesized and characterized. In addition, a new ligand, 3,5-bis(1,2,4-triazol-1-ylmethyl)toluene (1), was synthesized and full characterized. The complexes were obtained as air-stable solids and characterized by melting point, electrical conductivity, thermogravimetric analysis, and Raman, infrared and ultraviolet/visible spectroscopy. The analyses and spectral data showed that complexes 3–7 had 1:1 (M:L) stoichiometries and octahedral geometries, while 2 had a 1:2 (M:L) ratio, which was supported by DFT calculations. The complexes and their respective ligands were evaluated against bacterial and fungal strains with clinical relevance. All the complexes showed higher antibacterial and antifungal activities than the free ligands. The complexes were more active against fungi than against bacteria. The activities of the chromium complexes against Candida tropicalis are of great interest, as they showed minimum inhibitory concentration 50 (MIC50) values between 7.8 and 15.6 μg mL−1. Complexes 5 and 6 showed little effect on Vero cells, indicating that they are not cytotoxic. These results can provide an important platform for the design of new compounds with antibacterial and antifungal activities.

scholarly journals Synthesis, Characterization and Biological Activity Study of New Compounds Tetrazole Derivatives Azo-Schiff Base

2019 ◽  
Vol 25 (103) ◽  
pp. 68-89
Author(s):  
Hiba Ibrahim Abdulla AL-Joubory ◽  
Khalid Mohamad Motny Al-janaby
Keyword(s):  
Biological Activity ◽  
Schiff Base ◽  
Pathogenic Bacteria ◽  
Diazonium Salt ◽  
Aldehyde Group ◽  
Spectroscopic Techniques ◽  
Phenyl Hydrazine ◽  
Ft Ir ◽  
New Compounds ◽  
Tetrazole Derivatives

This work included synthesis of azo dye (H1) by the reaction of diazonium salt to sulfacetamide with 4-hydroxy benzaldehyde at (0-5) oC  and synthesis of schiff base (H2-H6) through reaction substituted aromatic amine (aniline, 4-nitro aniline, 4-chloro aniline, 4-amino benzoic acid and phenyl hydrazine)  with aldehyde group in azo compound (H1) in ethanol compounds (H2-H6) and tetrazole derivatives prepared by reaction schiff base with sodium azide in ethanol compounds (H7-H11) and characterization by using spectroscopic techniques Uv/Vis, FT-IR, C.H.N. and H1-NMR of some the prepared compounds using DMSO-d6 a solvent, in addition melting point and determination a purity of TLC, and this work consists a study of biological activity for the some prepared compounds against four types of pathogenic bacteria and know to be resistant to anti biotic.

scholarly journals The structural features and biological activity of Candida spec. yeast mannans

1995 ◽  
Vol 11 (3-4) ◽  
pp. 88-95 ◽  
Author(s):  
A. G. Kovalenko ◽  
A. S. Shashkov ◽  
V. N. Vasiljev ◽  
T. A. Telegeeva
Keyword(s):  
Biological Activity ◽  
Structural Features

QSAR Analysis of Saquinavir Analogues (Peptidomimetics) as Potent HIV‐Protease Inhibitors

2012 ◽  
Vol 2 (3) ◽  
pp. 118-127
Author(s):  
Vandana Saini ◽  
Ajit Kumar
Keyword(s):  
Biological Activity ◽  
Quantitative Structure Activity Relationship ◽  
Structural Features ◽  
Partial Least Square ◽  
Least Square ◽  
Activity Prediction ◽  
Qsar Analysis ◽  
Qsar Studies ◽  
Physicochemical Descriptors ◽  
Qsar Models

The correlation of structural features with the biological activity has always played an important role in drug designing process. The present paper discussesthe 2D‐ and 3D‐ Quantitative structure activity relationship (QSAR) studies, performed on a series of compounds related to saquinavir, an established HIV‐protease inhibitor (PI). The analysis was done on structure based calculations using various methods of QSAR like multiple linear regression (MLR), k‐nearest neighbour (k‐NN) and partial least square (PLS), to establish QSAR models for biological activity prediction of unknown compounds. A total of 27 peptidomimetics (Saquinavir analogues) were used for the study and models were developed using a training set of 22 compounds and test set of 5 compounds. The r2 value of 0.959 and crossvalidated r2 (q2) of 0.926 was obtained when models were generated using physicochemical descriptors during 2D‐QSAR analysis. In case of 3D‐QSAR analysis, database alignment of all compounds was done by field fit of steric and electrostatic molecular fields. 3D‐QSAR models generated showed r2 of 0.81 when steric and electrostatic fields were considered as basis of model generation. The meaningful information obtained from the study can be used for the design of saquinavir analogues having better inhibitory activity for HIV‐protease. Also, the QSAR models generated can be very useful to predict the HIV‐PIs and also for virtual screening for identification of new lead molecules.

The diverse bioactivity of α-mangostin and its therapeutic implications

2021 ◽  
Vol 13 (19) ◽  
pp. 1679-1694
Author(s):  
Tejashri Chavan ◽  
Aaron Muth
Keyword(s):  
Biological Activity ◽  
Natural Product ◽  
Secondary Metabolite ◽  
Bacterial Growth ◽  
Biological Effects ◽  
Structural Features ◽  
Therapeutic Implications ◽  
Specific Disease ◽  
Disease States ◽  
Key Pathways

α-Mangostin is a xanthone natural product isolated as a secondary metabolite from the mangosteen tree. It has attracted a great deal of attention due to its wide-ranging effects on certain biological activity, such as apoptosis, tumorigenesis, proliferation, metastasis, inflammation, oxidation, bacterial growth and metabolism. This review focuses on the key pathways directly affected by α-mangostin and how this varies between disease states. Insight is also provided, where investigated, into the key structural features of α-mangostin that produce these biological effects. The review then sheds light on the utility of α-mangostin as a investigational tool for certain diseases and demonstrate how future derivatives may increase selectivity and potency for specific disease states.

scholarly journals Terpenoids and Sterols from Some Japanese Mushrooms

2014 ◽  
Vol 9 (3) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Yasunori Yaoita ◽  
Masao Kikuchi ◽  
Koichi Machida
Keyword(s):  
Lentinula Edodes ◽  
Chemical Constituents ◽  
Structural Features ◽  
Tricholoma Matsutake ◽  
Pholiota Nameko ◽  
The Past ◽  
Polyporus Umbellatus ◽  
Hericium Erinaceum ◽  
New Compounds ◽  
Hypsizigus Marmoreus

Over the past twenty years, our research group has been studying the chemical constituents of mushrooms. From nineteen species, namely, Amanita virgineoides Bas (Amanitaceae), Daedaleopsis tricolor (Bull.: Fr.) Bond. et Sing. (Polyporaceae), Grifola frondosa (Fr.) S. F. Gray (Polyporaceae), Hericium erinaceum (Bull.: Fr.) Pers. (Hericiaceae), Hypsizigus marmoreus (Peck) Bigelow (Tricholomataceae), Lactarius piperatus (Scop.: Fr.) S. F. Gray (Russulaceae), Lentinula edodes (Berk.) Sing. (Pleurotaceae), Lyophyllyum connatum (Schum.: Fr.) Sing. (Tricholomataceae), Naematoloma sublateritium (Fr.) Karst. (Strophariaceae), Ompharia lapidescens Schroeter (Polyporaceae), Panellus serotinus (Pers.: Fr.) Kuhn. (Tricholomataceae), Pholiota nameko (T. Ito) S. Ito et Imai in Imai (Strophariaceae), Pleurotus eringii (DC.: Fr.) Quel. (Pleurotaceae), Polyporus umbellatus Fries (Polyporaceae), Russula delica Fr. (Russulaceae), Russula sanguinea (Bull.) Fr. (Russulaceae), Sarcodon aspratus (Berk.) S. Ito (Thelephoraceae), Tricholoma matsutake (S. Ito et Imai) Sing. (Tricholomataceae), and Tricholoma portentosum (Fr.) Quel. (Tricholomataceae), we isolated eight new sesquiterpenoids, six new meroterpenoids, three new triterpenoids, and twenty eight new sterols. In this review, structural features of these new compounds are discussed.

scholarly journals Characterization of Ionic Liquid Lignins Isolated from Spruce Wood with 1-Butyl-3-methylimidazolium Acetate and Methyl Sulfate and Their Binary Mixtures with DMSO

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2479 ◽  
Author(s):  
Artyom V. Belesov ◽  
Anton V. Ladesov ◽  
Ilya I. Pikovskoi ◽  
Anna V. Faleva ◽  
Dmitry S. Kosyakov
Keyword(s):  
Ionic Liquids ◽  
Binary Mixtures ◽  
Plant Biomass ◽  
High Resolution Mass Spectrometry ◽  
Covalent Binding ◽  
Structural Features ◽  
Size Exclusion ◽  
Hydroxyl Groups ◽  
Spruce Wood

Ionic liquids (ILs) based on 1-butyl-3-methylimidazolium (bmim) cation have proved to be promising solvents for the fractionation of plant biomass with the production of cellulose and lignin. This study deals with the characterization of lignins isolated from coniferous (spruce) wood using [bmim]OAc and [bmim]MeSO4 ionic liquids and their binary mixtures with DMSO (80:20). Molecular weight distributions, functional composition, and structural features of IL lignins were studied by size-exclusion chromatography, NMR spectroscopy (1D and 2D) and atmospheric pressure photoionization high-resolution mass spectrometry. It was shown that the interaction of ILs with lignin leads to significant chemical changes in the biopolymer; a decrease in the degree of polymerization and in the content of free phenolic hydroxyl groups due to alkylation, the disappearance (in the case of [bmim]OAc) of carbonyl groups and a significant destruction of β-O-4 bonds. The chemical reactions between lignin and 1-butyl-3-methylidazolium cation with covalent binding of ionic liquids or products of their decomposition is evidenced by the presence of a large number of nitrogen-containing oligomers in IL lignins.

scholarly journals Chemical Profile and Biological Activity of Cherimoya (Annona cherimola Mill.) and Atemoya (Annona atemoya) Leaves

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2612 ◽  
Author(s):  
Giuseppe Mannino ◽  
Carla Gentile ◽  
Alessandra Porcu ◽  
Chiara Agliassa ◽  
Fabio Caradonna ◽  
...  
Keyword(s):  
Biological Activity ◽  
Dietary Supplements ◽  
Redox Balance ◽  
Scientific Data ◽  
Chemical Profile ◽  
Tropical Plants ◽  
Annona Cherimola ◽  
Hepg2 Cell Lines ◽  
Preventive Effects ◽  
Potential Use

Annona cherimola (Cherimoya) and Annona atemoya (Atemoya) are tropical plants known for their edible fruit. Scientific data suggest that their leaves, used in traditional medicine in the form of teas or infusions without evidence of toxicity, contain several bioactive compounds. However, only Annona muricata among all the Annona species is currently used in the nutraceutical field, and its dried leaves are marketed for tea preparation. In this work, we explored the nutraceutical potential of Atemoya and Cherimoya leaves, by evaluating their chemical profile and functional properties. Phytochemical analyses showed large amounts of phenolic compounds, in particular proanthocyanidins, and identified 18 compounds, either flavonoids or alkaloids. Concerning biological activity, we found antioxidative properties correlated with polyphenols, and antiproliferative activity against HeLa and HepG2 cell lines correlated with alkaloids. The obtained results demonstrate the potential use of Annona cherimola leaves for the preparation of dietary supplements aimed to promote the physiological redox balance. Moreover, the varietal comparison suggests that two commercial cultivars (Campas and White) and the local Torre 1, better suit this purpose. On the other hand, among the studied cultivars, Campas and Torre 1 are also the richest in alkaloids and, in consideration of the anti-proliferative properties of their extracts, dietary supplements based on these cultivars might also have chemo-preventive effects.

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