scholarly journals Copper(II) Complexes of 4, 4- Diaminodiphenylsulphone: Synthesis, Characterization and Biological Studies

2009 ◽  
Vol 6 (s1) ◽  
pp. S311-S323 ◽  
Author(s):  
Adedibu C. Tella ◽  
Joshua A. Obaleye
Keyword(s):  
Metal Ion ◽  
Biological Activities ◽  
Free Ligand ◽  
Albino Rats ◽  
Copper Salts ◽  
Tetrahedral Configuration ◽  
Biological Studies ◽  
Esherichia Coli ◽  
Liver And Kidney ◽  
Kidney Liver

Five complexes of copper(II) 4,4-diaminodiphenylsulphone have been synthesized. Copper salts of counter ion (sulphate, nitrate, chloride) and different reaction media (solvents) were used for the synthesis. The complexes varied in colour and composition. The compounds were characterized by conductivity, IR, UV, NMR and mass spectroscopies. The ligand coordinated to metal ion in a monodentate and bidentate manner. All the five complexes have tetrahedral configuration. The biological activities data showed that the complexes are more active againstEsherichia coli, Klebbsiella pneumoniaeandStaphylococcus aureusthan the free ligand (4,4- diaminodiphenyl sulphone). Antimalaria activities of the complexes and the ligand were investigated using mice infected withPlasmodium berghei. All the complexes exhibited lower activity than the ligand and chloroquine. The effect of administration of the complexes on alkaline phosphatase activities of kidney, liver and serum of Albino rats were investigated. The serum ALP activity showed no significant change (P> 0.05), suggesting non-damaging effect on the plasma membrane of liver and kidney cells.

Does rosmarinic acid treatment have protective role against sepsis-induced oxidative damage in Wistar Albino rats?

2016 ◽  
Vol 35 (8) ◽  
pp. 877-886 ◽  
Author(s):  
M Bacanlı ◽  
S Aydın ◽  
G Taner ◽  
HG Göktaş ◽  
T Şahin ◽  
...  
Keyword(s):  
Dna Damage ◽  
Oxidative Damage ◽  
Rosmarinic Acid ◽  
Biological Activities ◽  
Albino Rats ◽  
Repair Capacity ◽  
Tnf Α ◽  
Liver And Kidney ◽  
Wistar Albino Rats ◽  
Α Level

Reactive oxygen species are believed to be involved in the development of sepsis. Plant-derived phenolic compounds are thought to be possible therapeutic agents against sepsis because of their antioxidant properties. Rosmarinic acid (RA) is a phenolic compound commonly found in various plants, which has many biological activities including antioxidant activity. The aim of this study was to investigate the effects of RA on sepsis-induced DNA damage in the lymphocytes and liver and kidney cells of Wistar albino rats by alkaline comet assay with and without formamidopyrimidine DNA glycosylase protein. The oxidative stress parameters such as superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) activities and total glutathione (GSH) and malondialdehyde (MDA) levels in the liver and kidney tissues and an inflammatory cytokine, tumor necrosis factor α (TNF-α) level in plasma were also evaluated. It is found that DNA damage in the lymphocytes, livers, and kidneys of the RA-treated rats was significantly lower than that in the sepsis-induced rats. RA treatment also decreased the MDA levels and increased the GSH levels and SOD and GSH-Px activities in the livers and kidneys of the sepsis-induced rats. Plasma TNF-α level was found to be decreased in the RA-treated rats. It seems that RA might have a role in the attenuation of sepsis-induced oxidative damage not only by decreasing the DNA damage but also by increasing the antioxidant status and DNA repair capacity of the animals.

scholarly journals Synthesis, Spectroscopic Characterization, and Biological Activities of New Binuclear Co(II), Ni(II), Cu(II), and Zn(II) Diimine Complexes

Crystals ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 300
Author(s):  
Ahmed Gaber ◽  
Arafa A. M. Belal ◽  
Ibrahim M. El-Deen ◽  
Nader Hassan ◽  
Rozan Zakaria ◽  
...  
Keyword(s):  
Metal Complexes ◽  
Metal Atom ◽  
Biological Activities ◽  
Free Ligand ◽  
Molar Conductivity ◽  
Stoichiometric Ratio ◽  
Biological Studies ◽  
Major Interest ◽  
Diimine Ligand ◽  
Diimine Complexes

Metal-ligand complexes have attracted major interest due to their potential medical applications as anticancer agents. The work described in the current article aimed to synthesize, spectroscopic, thermal, and biological studies of some metal-diimine complexes. A diimine ligand, namely 2-{[2-(4-chlorophenyl)-2-hydroxyvinyl]-hydrazonomethyl}phenol (diim) was prepared via the reaction of p-chlorophenacyl bromide with hydrazine hydrate in ethanol, then condensation was completed with 2-hydroxybenzaldehyde in acetic acid. The Co(II), Ni(II), Cu(II), and Zn(II) complexes were prepared with a metal:ligand stoichiometric ratio of (2:1). 1H-NMR, UV-Vis, FTIR spectroscopic data, molar conductivity measurements, and microanalytical data (carbon, hydrogen, nitrogen, and halogen) were used for characterization of the formed ligand and its metal complexes. It was found that the diimine ligand act as tetradentate fashion. The non-electrolytic character for all the complexes was proved by molar conductivity. The first metal atom of the synthesized binuclear diimine complexes coordinates with the nitrogen of hydrazine group and oxygen of OH group. While, the second metal atom coordinates with the other nitrogen atom of the hydrazine group and oxygen of phenolic group. All the synthesized metal complexes have a six-coordinated except for Zn(II) has four-coordinated. Thermogravimetric analysis and its differential analysis were done to discuss the thermal degradation of the free ligand and its metal complexes. Molecular docking calculation showed that the diimine ligand is a good inhibitor for breast cancer 3hb5 and 4o1v kidney cancer proteins. Additionally, these compounds were evaluated as antibacterial and antifungal agents.

Synthesis, Characterization and Biological Studies of Some Transition Metal Complexes with Pyrazine Schiff Base Hydra zone Ligand

2020 ◽  
Vol 15 (2) ◽  
pp. 61-72
Keyword(s):  
Metal Complexes ◽  
Metal Ion ◽  
Metal Salt ◽  
Free Ligand ◽  
Spectroscopic Studies ◽  
Fungal Species ◽  
Molar Conductance ◽  
Central Metal ◽  
Biological Studies

New pyrazine carbohydra zone ligand N'-(1-(5-chloro-2-hydroxyphenyl) ethylidene) pyrazine-2-carbohydrazide (H2L), prepared by the condensation of equimolar amounts of pyrazine-2-carbohydrazide with 2-hydroxy-5-chloroacetophenone in methanol, reacts with suitable metal salt precursors to give complexes of two general formulae: [M(HL)(Cl)(H2O)2] {M = Mn(II), Co(II), Ni(II) and Cu(II)} and [M(L)(H2O)] {M = Zn(II) and Cd(II)}. Structure of ligand was confirmed by elemental analysis, IR, 1H and 13C NMR and mass spectroscopy, while synthesized complexes were additionally characterized by magnetic susceptibility measurements, molar conductivity measurements, XRD, ESR (for Cu(II)), SEM and thermogravimetric analysis. Spectroscopic studies confirmed a tridentate ONO donor behavior of the ligand towards the central metal ion. The molar conductance (12–17 W–1 cm2 mol–1) measurements in DMSO indicated non-electrolytic nature. Thermal behavior of the complexes suggests their extended stability and the thermal decomposition generally proceeds via partial loss of the organic moiety and ends with the formation of respective metal oxide as a final product. Various kinetic and thermodynamic parameters were evaluated using the Coats-Redfern method. The solid-state electrical conductivity of the complexes measured in the temperature range 303-463 K suggested their semiconducting behavior. The ligand and its metal complexes were screened in vitro for their antibacterial activity against the Gram-positive bacteria S. aureus and B. subtilis, the Gram-negative bacteria E. coli and S. typhi and the fungi C. albicans and A. niger. The obtained results indicated improved activity of the complexes compared to the free ligand against all studied bacterial and fungal species.

scholarly journals Acute and Subchronic Toxicity Profile of Euphorbia pulcherrima Methanol Extract on Wistar Albino Rats

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
H. B. Sharif ◽  
M. D. Mukhtar ◽  
Y. Mustapha ◽  
Gabi Baba ◽  
A. O. Lawal
Keyword(s):  
Kidney Function ◽  
Methanol Extract ◽  
Normal Values ◽  
Lethal Dose ◽  
Albino Rats ◽  
Subchronic Toxicity ◽  
Mean Values ◽  
Liver And Kidney ◽  
Wistar Albino Rats ◽  
Kidney Liver

This work was designed to evaluate the acute and subchronic toxicity of E. pulcherrima methanol extract. Mean lethal dose (LD50) and subchronic toxicity were determined using Lorke’s method to assess the effect of the extract on kidney and liver functions along histopathology assessment of the liver and kidney, respectively. The LD50 determined was 3807.89 mg/kg both orally and intraperitoneally. The kidney function parameters indicated elevation of the serum urea above the normal value in both control and the group treated with 10 mg/kg of the extract with mean values of 7.92 ± 1.19 and 7.86 ± 1.14 mMol/L, respectively. The creatinine and electrolytes were within the normal values. The results of ALAT, ASAT, ALP, T protein albumin, and bilirubin in all cases were within the normal values. Kidney, liver function parameters, and relative organ weight were statistically insignificant across all groups. This shows that various concentrations of E. pulcherrima extract did not influence negatively the liver and kidney function parameters. Further studies are required to rule out the observed mild hepatic histological changes among a few members of the groups treated with 100 and 1000 mg/kg/day and any possible hepatoprotective and nephron-protective potential the extract may possess.

Recent Developments on Synthesis of Indole Derivatives Through Green Approaches and Their Pharmaceutical Applications

2020 ◽  
Vol 24 (22) ◽  
pp. 2665-2693
Author(s):  
Dipayan Mondal ◽  
Pankaj Lal Kalar ◽  
Shivam Kori ◽  
Shovanlal Gayen ◽  
Kalpataru Das
Keyword(s):  
Biological Activities ◽  
Synthetic Methods ◽  
Pharmaceutical Chemistry ◽  
Indole Derivatives ◽  
Biological Studies ◽  
Recent Developments ◽  
Pharmaceutical Industries ◽  
Green Methodology ◽  
Conventional Methods ◽  
High Yields

Indole moiety is often found in different classes of pharmaceutically active molecules having various biological activities including anticancer, anti-viral, anti-psychotic, antihypertensive, anti-migraine, anti-arthritis and analgesic activities. Due to enormous applications of indole derivatives in pharmaceutical chemistry, a number of conventional synthetic methods as well as green methodology have been developed for their synthesis. Green methodology has many advantages including high yields, short reaction time, and inexpensive reagents, highly efficient and environmentally benign over conventional methods. Currently, the researchers in academia as well as in pharmaceutical industries have been developing various methods for the chemical synthesis of indole based compounds via green approaches to overcome the drawbacks of conventional methods. This review reflects the last ten years developments of the various greener methods for the synthesis of indole derivatives by using microwave, ionic liquids, water, ultrasound, nanocatalyst, green catalyst, multicomponent reaction and solvent-free reactions etc. (please see the scheme below). Furthermore, the applications of green chemistry towards developments of indole containing pharmaceuticals and their biological studies have been represented in this review.

scholarly journals Utilization and simulation of innovative new binuclear Co(ii), Ni(ii), Cu(ii), and Zn(ii) diimine Schiff base complexes in sterilization and coronavirus resistance (Covid-19)

2021 ◽  
Vol 19 (1) ◽  
pp. 772-784
Author(s):  
Moamen S. Refat ◽  
Ahmed Gaber ◽  
Walaa F. Alsanie ◽  
Mohamed I. Kobeasy ◽  
Rozan Zakaria ◽  
...  
Keyword(s):  
Schiff Base ◽  
Molecular Docking ◽  
Metal Ions ◽  
Free Ligand ◽  
Schiff Base Complexes ◽  
Hydroxyl Groups ◽  
Binuclear Complexes ◽  
Central Metal ◽  
H Nmr ◽  
Biological Studies

Abstract This article aimed at the synthesis and molecular docking assessment of new diimine Schiff base ligand, namely 2-((E)-(2-((Z)-2-(4-chlorophenyl)-2-hydroxyvinyl)hydrazono) methyl)-6-methoxyphenol (methoxy-diim), via the condensation of 1-(4-chloro-phenyl)-2-hydrazino-ethenol compound with 2-((E)-(2-((Z)-2-(4-chlorophenyl)-2-hydroxy vinyl) hydrazono)methyl)-6-methoxyphenol in acetic acid as well as the preparation of new binuclear complexes of Co(ii), Ni(ii), Cu(ii), and Zn(ii). The following synthesized complexes were prepared in a ratio of 2:1 (metal/ligand). The 1H-NMR, UV-Vis, and FTIR spectroscopic data; molar conductivity measurements; and microanalytical, XRD, TGA/DTG, and biological studies were carried out to determine the molecular structure of these complexes. According to the spectroscopic analysis, the two central metal ions were coordinated with the diamine ligand via the nitrogen of the hydrazine and oxygen of the hydroxyl groups for the first metal ions and via the nitrogen of the hydrazine and oxygen of the phenol group for the second metal ions. Molecular docking for the free ligand was carried out against the breast cancer 3hb5-oxidoreductase and the 4o1v-protein binding kidney cancer and COVID-19 protease, and good results were obtained.

Update on Phytochemical and Biological Studies on Rocaglate Derivatives from Aglaia Species

Planta Medica ◽  
2021 ◽  
Author(s):  
Garima Agarwal ◽  
Long-Sheng Chang ◽  
Djaja Doel Soejarto ◽  
A. Douglas Kinghorn
Keyword(s):  
Biological Activities ◽  
Chemical Constituents ◽  
Protein Translation ◽  
Biological Properties ◽  
Translation Initiation Factor ◽  
Initiation Factor ◽  
Eukaryotic Translation ◽  
Ability To Act ◽  
Biological Studies ◽  
Phytochemical Constituents

AbstractWith about 120 species, Aglaia is one of the largest genera of the plant family Meliaceae (the mahogany plants). It is native to the tropical rainforests of the Indo-Australian region, ranging from India and Sri Lanka eastward to Polynesia and Micronesia. Various Aglaia species have been investigated since the 1960s for their phytochemical constituents and biological properties, with the cyclopenta[b]benzofurans (rocaglates or flavaglines) being of particular interest. Phytochemists, medicinal chemists, and biologists have conducted extensive research in establishing these secondary metabolites as potential lead compounds with antineoplastic and antiviral effects, among others. The varied biological properties of rocaglates can be attributed to their unusual structures and their ability to act as inhibitors of the eukaryotic translation initiation factor 4A (eIF4A), affecting protein translation. The present review provides an update on the recently reported phytochemical constituents of Aglaia species, focusing on rocaglate derivatives. Furthermore, laboratory work performed on investigating the biological activities of these chemical constituents is also covered.

Enzymatic Synthesis of Glycosphingolipids: A Review

Synthesis ◽  
2021 ◽  
Author(s):  
Qingjiang Li ◽  
Zhongwu Guo
Keyword(s):  
Signal Transduction ◽  
Enzymatic Synthesis ◽  
Biological Activities ◽  
Cell Interaction ◽  
Glycosidic Linkage ◽  
The Past ◽  
Biological Studies ◽  
Hydrophobic Lipid ◽  
Synthetic Methodologies ◽  
And Function

Glycosphingolipids (GSLs) are the major vertebrate glycolipids, which contain two distinctive moieties, a glycan and a ceramide, stitched together by a β-glycosidic linkage. The hydrophobic lipid chains of ceramide can insert into the cell membrane to form “lipid rafts” and anchor the hydrophilic glycan onto the cell surface to generate microdomains and function as signaling molecules. GSLs mediate signal transduction, cell interaction, and many other biological activities, and are also related to many diseases. To meet the need of biological studies, chemists have developed various synthetic methodologies to access GSLs. Among them, the application of enzymes to GSL synthesis has witnessed significant advancements in the past decades. This review summarizes briefly the history and progress of enzymatic GSL synthesis.

scholarly journals Synthesis, Spectral Characterization and Biological Activity of Metal(II) Complexes of 2,4,5-Trimethoxybenzaldehyde-S-Benzyldithiocarbazone

2019 ◽  
Vol 32 (1) ◽  
pp. 209-214
Author(s):  
Deepak Kumar ◽  
Arun Kumar Singh ◽  
Ajay Kumar ◽  
Dayanand Prasad ◽  
Vijay Kumar ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Metal Complexes ◽  
Metal Ion ◽  
Free Ligand ◽  
Azomethine Nitrogen ◽  
Octahedral Symmetry ◽  
Spectral Bands ◽  
Distorted Octahedral ◽  
And Staphylococcus Aureus

2,4,5-Trimethoxybenzaldehyde was condensed with S-benzyldithiocarbazate to give Schiff base 2,4,5-trimethoxy benzaldehyde-S-benzyldithiocarbazone (BBTC), which was used for complexation with Mn(II), Fe(II) and Co(II) metal ions. The complexes were formulated as M(BBTC)2X2 where X is Cl−, NO3− and CH3COO−. The FTIR spectra of the metal complexes in comparison to that of free ligand suggested the coordination through azomethine nitrogen and thion sulphur forming six membered chelating with metal ion. The magnetic susceptibility and electronic spectral bands revealed octahedral symmetry (Oh) around Mn(II) but tetragonally distorted octahedral symmetry (D4h) of Fe(II) and Co(II) complexes. The positive value of Dt for Fe(II) (68.42-135.2 cm-1) and Co(II) (263-280 cm-1) clearly indicated elongation along z-axis in these complexes which was also supported by the less value of Dq(z) than Dq(xy) for the metal complexes. The ligand as well as its metal complexes have been found active against the bacteria Escherichia coli and Staphylococcus aureus, and antibacterial activity of the free ligand has been observed to have enhanced in metal complexes.

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