Synthesis and Antibacterial Activity of Rhodanine-Based Azo Dyes and Their Use as Spectrophotometric Chemosensor for Fe3+ Ions

Chemosensors ◽  
2020 ◽  
Vol 8 (1) ◽  
pp. 16 ◽  
Author(s):  
Dana Akram ◽  
Ismail A. Elhaty ◽  
Shaikha S. AlNeyadi
Keyword(s):  
Pathogenic Bacteria ◽  
Biological Activities ◽  
Bacterial Species ◽  
High Sensitivity ◽  
Azo Compounds ◽  
Molar Ratio ◽  
Spectroscopic Techniques ◽  
Reference Drug ◽  
Physiochemical Properties ◽  
Design And Synthesis

This research includes the design and synthesis of new derivatives for rhodanine azo compounds (4a–c) containing a naphthalene ring. Physiochemical properties of the synthesized compounds were determined by their melting points, FTIR, 1H-NMR, 13C-NMR, and elemental analysis spectroscopic techniques. The biological activities of the newly prepared azo rhodanine compounds were evaluated against some pathogenic bacteria using three different bacterial species including (Escherichia coli., Pseudomonas aeruginosa, Staphylococcus aureus) and compared with amoxicillin as a reference drug. The results showed that our compounds have moderate-to-good vital activity against the mentioned pathogenic bacteria. The selectivity and sensitivity of the newly prepared rhodanine azo compounds with transition metals Co2+, Cu2+, Zn2+, Ni2+, and Fe3+ were studied using UV–vis and fluorescence spectroscopy techniques. Among the synthesized azos, azo 4c showed affinity toward Fe3+ ions with an association constant of 4.63 × 108 M−1. Furthermore, this azo showed high sensitivity toward Fe3+ ions with detection limits of 5.14 µM. The molar ratio and Benesi–Hildebrand methods confirmed the formation of complexes between azo 4c and Fe3+ with 1:2 binding stoichiometry. Therefore, azo 4c showed excellent potential for developing efficient Fe3+ chemosensors.

Design and Synthesis of Novel Thiosemicarbazones as Potent Anti-breast Cancer Agents

2019 ◽  
Vol 16 (4) ◽  
pp. 446-452 ◽  
Author(s):  
Mashooq Ahmad Bhat ◽  
M. Al-Tahhan ◽  
Mohamed A. Al-Omar ◽  
Ahmed M. Naglah ◽  
Abdullah Al-Dhfyan
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Side Population ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Inhibition Assay ◽  
Reference Drug ◽  
Design And Synthesis ◽  
Pure Compounds ◽  
Mcf 7

Background: Thiosemicarbazones and its derivatives received a great pharmaceutical importance due to their prominent biological activities. Methods: A series of disubstituted thiosemicarbazone derivatives (1-12) were designed and synthesized as pure compounds in good yield. All the synthesized compounds were analyzed by spectral data. The anticancer activity of all the compounds was performed against breast cancer MCF-7 and MDA-MB-231 cell lines. Results: Most of the compounds showed activity against breast cancer MCF-7 and MDA-MB-231 cell lines with (IC50 = 12.25 µM ‒ 185.35 µM) and (IC50 = 12.97 µM ‒ 107.33 µM), respectively. Compound 9 presented (IC50 = 12.76 µM and 12.97 µM) against MCF-7 and MDA-MB-231 cell lines, respectively. Conclusion: Compound 9, was found to exhibit significant anti-breast cancer activity. This compound was further evaluated for side population percent inhibition assay on the breast cancer cell line MCF-7 at 5 and 10 µM concentration. It showed superiority to block side population by more than 80% at 5 μM concentration compared to the reference drug verapamil.

scholarly journals Synthesis, spectral characterization and biological activities of Ag(I), Pt(IV) and Au(III) complexes with novel azo dye ligand (N,N,O) derived from 2-amino-6-methoxy benzothiazole

2022 ◽  
Author(s):  
Hussein A. K. Kyhoiesh ◽  
Khalid J. Al-Adilee
Keyword(s):  
Crystal Structure ◽  
Endometrial Cancer ◽  
Nitrogen Atom ◽  
Metal Complexes ◽  
Cancer Cells ◽  
Azo Dye ◽  
Biological Activities ◽  
Antifungal Drugs ◽  
Azo Compounds ◽  
Spectroscopic Techniques

Abstract The novel ligand 2-[2'-(6-methoxybenzothiazolyl)azo]-3,5-dimethyl benzoic acid (6-MBTAMB), derived from 2-amino-6-methoxy benzothiazole, has been used to synthesize a series of new metal complexes of Ag(I), Pt(IV) and Au(III). The metal complexes were characterized by elemental analyses (CHNS), molar conductivity, crystal structure (XRD), spectroscopic techniques: FT-IR, 1H NMR, 13C NMR, UV-Vis, mass spectra, thermal analysis (TG-DTA), FE-SEM and magnetic properties. Results confirmed that the azo dye ligand behaves a tridentate and coordinates to the metal ion via nitrogen atom of azomethine group of heterocyclic benzothiazole ring, nitrogen atom of the azo group which is the farthest of the benzothiazole molecule and carboxylic oxygen. Antimicrobial properties of all newly synthesized azo compounds are also demonstrated against bacterial pathogenic organisms and fungi. These complexes are more effective against bacteria and less effective against fungi compared to standard antibacterial drugs (Novobiocin) and antifungal drugs (Cycloheximide). By using the DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging test, it was discovered that the complexes had good antioxidant properties. In addition, the (6-MBTAMB) and metal complexes were docked with the crystal structure of FGF Receptor 2 (FGFR2) kinase domain harboring the pathogenic gain of function K659E mutation identified in endometrial cancer using the Molecular Operating Environment module (MOE). In vitro studies on human endometrial cancer cell lines (MFE-296) as well as healthy human umbilical vein endothelial cells (HUVEC) show uptake of the intact compounds by the cancer cells and increased activity against the cancer cells.

scholarly journals Synthesis, Characterization, and Biological Activity of Nickel (II) and Palladium (II) Complex with Pyrrolidine Dithiocarbamate (PDTC)

2016 ◽  
Vol 2016 ◽  
pp. 1-6 ◽  
Author(s):  
Sk Imadul Islam ◽  
Suvendu Bikash Das ◽  
Sutapa Chakrabarty ◽  
Sudeshna Hazra ◽  
Akhil Pandey ◽  
...  
Keyword(s):  
Pathogenic Bacteria ◽  
Free Ligand ◽  
Molar Ratio ◽  
Palladium Acetate ◽  
Pyrrolidine Dithiocarbamate ◽  
Spectroscopic Methods ◽  
Spectroscopic Techniques ◽  
Streptococcus Pneumonia ◽  
Square Planar ◽  
Bsa Interaction

The synthesis of square planar Ni(II) and Pd(II) complexes with pyrrolidine dithiocarbamate (PDTC) was characterized by elemental, physiochemical, and spectroscopic methods. Two complexes were prepared by the reaction of nickel acetate and palladium acetate with pyrrolidine dithiocarbamate (PDTC) in 1 : 2 molar ratio. The bovine serum albumin (BSA) interaction with complexes was examined by absorption and fluorescence spectroscopic techniques at pH 7.4. All the spectral data suggest that coordination of the pyrrolidine dithiocarbamate (PDTC) takes place through the two sulphur atoms in a symmetrical bidentate fashion. All the synthesized compounds were screened for their antimicrobial activity against some species of pathogenic bacteria (Escherichia coli, Vibrio cholerae, Streptococcus pneumonia, and Bacillus cereus). It has been observed that complexes have higher activity than the free ligand.

scholarly journals Multiplexed Bead-Based Mesofluidic System for Detection of Food-Borne Pathogenic Bacteria

2009 ◽  
Vol 75 (21) ◽  
pp. 6647-6654 ◽  
Author(s):  
Sheng-Quan Jin ◽  
Bin-Cheng Yin ◽  
Bang-Ce Ye
Keyword(s):  
Pathogenic Bacteria ◽  
Bacterial Species ◽  
Simultaneous Detection ◽  
High Sensitivity ◽  
Microarray Scanner ◽  
Food Borne ◽  
Pcr Products ◽  
Meat Samples ◽  
Multiple Pathogens ◽  
Modified Oligonucleotide

ABSTRACT In the present study, a simple and rapid multiplexed bead-based mesofluidic system (BMS) was developed for simultaneous detection of food-borne pathogenic bacteria, including Staphylococcus aureus, Vibrio parahaemolyticus, Listeria monocytogenes, Salmonella, Enterobacter sakazakii, Shigella, Escherichia coli O157:H7, and Campylobacter jejuni. This system is based on utilization of isothiocyanate-modified microbeads that are 250 μm in diameter, which were immobilized with specific amino-modified oligonucleotide probes and placed in polydimethylsiloxane microchannels. PCR products from the pathogens studied were pumped into microchannels to hybridize with the oligonucleotide-modified beads, and hybridization signals were detected using a conventional microarray scanner. The short sequences of nucleic acids (21 bases) and PCR products characteristic of bacterial pathogens could be detected at concentrations of 1 pM and 10 nM, respectively. The detection procedure could be performed in less than 30 min with high sensitivity and specificity. The assay was simple and fast, and the limits of quantification were in the range from 500 to 6,000 CFU/ml for the bacterial species studied. The feasibility of identification of food-borne bacteria was investigated with samples contaminated with bacteria, including milk, egg, and meat samples. The results demonstrated that the BMS method can be used for effective detection of multiple pathogens in different foodstuffs.

scholarly journals Bacterial causes of upper & lower respiratory tract infection in Sheep

2005 ◽  
Vol 29 (1) ◽  
pp. 1-10
Author(s):  
Jamal Salman Ali
Keyword(s):  
Tract Infection ◽  
Respiratory Tract ◽  
Nasal Cavity ◽  
Respiratory Tract Infection ◽  
Lower Respiratory Tract Infection ◽  
Lower Respiratory Tract ◽  
Pathogenic Bacteria ◽  
Bacterial Species ◽  
High Sensitivity ◽  
Hemorrhagic Lesion

This study was designed to investigate the bacterial species that induceupper and lower respiratory tract infection in sheep, and to find out anyrelationship which may exist between them.Therefore two groups of sheep were employed. The first group wassuffering from certain respiratory signs. While the second group was apparentlyhealthy. Each group included 50 sheep. Research samples were collected for aperiod of six months from AL-Shulla Abattoir.Microbiological investigation indicated the isolation of certainmicroorganisms from all animals in both groups from nasal cavity, and from 34lungs of the first group and 16 lungs of the second group. The number of isolatesfrom the nasal cavity, were 200 from different species ,43 isolates from thebronchioles and 70 from the lungs tissue. On the other hand the number ofbacterial isolates from the nasal cavity, bronchioles and the lung tissue of thefirst group were 113, 29 and 55 respectively.The study revealed the isolation of potentially pathogenic bacteria from thelower respiratory system of both groups, these bacteria were namely Pasteurellahaemolytica of serotype (A2), Niesseria spp. and Corynebacterium pyogenes,the number of isolates were 6 for each, and 8 isolates of Staphylococcus aureus.These bacteria were also isolated from the nasal cavity. The isolation of thesebacteria from the nasal strongly suggested their presence in the lungs and theprobable role in lesion formation.Animal inoculation were performed to study the virulence of P.haemolytica which caused certain hemorrhagic lesion in the lung , liver andkidney, with areas of necrosis in the lungs of the experimentally inoculatedrabbit, and caused death in mice. While the inoculation of C. ovis caused thedeath of rabbits within 72 hours, together with the presence of multipleabscessation on the internal organs and abdomenal wall.Sensitivity tests indicated a high sensitivity of most isolates to Gentamicin,Erythromycin and Kanamycin.

scholarly journals Synthesis, Spectral Characterization and Biological Activities of Co(II) and Ni(II) Mixed Ligand Complexes

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 823
Author(s):  
P. Manimaran ◽  
S. Balasubramaniyan ◽  
Mohammad Azam ◽  
D. Rajadurai ◽  
Saud I. Al-Resayes ◽  
...  
Keyword(s):  
Metal Complexes ◽  
Pathogenic Bacteria ◽  
High Efficiency ◽  
Biological Activities ◽  
Visible Spectrum ◽  
Fungal Species ◽  
Molar Conductance ◽  
Molar Ratio ◽  
Cell Parameters

2,4-Dinitrophynylhydrazine and two thiocyanate ions in a (M:L1:L2) 1:2:2 molar ratio was synthesized in the complexes of Co(II) and Ni(II). The prepared compounds were identified through a C.H.N.S. analysis, conductivity measurements, powder X-ray diffraction (PXRD), the infrared spectrum, and a UV-visible spectrum analysis, in addition to the magnetic properties being measured. The measurements of the molar conductance implieda nonelectrolytic nature of compounds Co(II) and Ni(II). The magnetic susceptibility, as well as electronic spectra, represented all the metal complexesthroughoctahedral geometry, respectively. The PXRD patterns suggested that all the complexes were an orthorhombic system with unit cell parameters. The in-vitro biological activity of the ligand and the metal complexes were screened against the Gram-positive and negative pathogenic bacteria Staphylococcus aureus, Bacillus subtilis, Pseudomonas, aeruginosa and Escherichia coli, as well as the fungal species of Aspergillusniger and Candida albicans.Thus, the metal complexes showeda high efficiency of antimicrobial activity compared with the ligand. Furthermore, applications of the ligand, as well as the metal complexes, were tested for in-vitro antioxidant potential in aDPPH assay. The results showed that the activity of the metal complexes with the in-vitro antioxidant was more active than that of 2,4-dinitrophenylhydrazine(DNPH).

Biological Activities and Physiochemical Properties of Gangwon-do Endemic Makjang Products

2015 ◽  
Vol 44 (6) ◽  
pp. 862-873 ◽  
Author(s):  
Byoung-Mok Kim ◽  
Jee-Hee Jung ◽  
Ji-Hoon Lim ◽  
Min-Jeong Jung ◽  
Jae-Whung Jeong ◽  
...  
Keyword(s):  
Biological Activities ◽  
Physiochemical Properties

Antimicrobial properties of actively purified secondary metabolites isolated from different marine organisms

2020 ◽  
Vol 21 ◽  
Author(s):  
Nilushi Indika Bamunu Arachchige ◽  
Fazlurrahman Khan ◽  
Young-Mog Kim
Keyword(s):  
Secondary Metabolites ◽  
Pathogenic Bacteria ◽  
Antimicrobial Agents ◽  
Bacterial Species ◽  
Antimicrobial Properties ◽  
Antimicrobial Effect ◽  
Cost Effective ◽  
Resistance Mechanisms ◽  
Marine Organisms ◽  
Antimicrobial Compounds

Background: The treatment of infection caused by pathogenic bacteria becomes one of the serious concerns globally. The failure in the treatment was found due to the exhibition of multiple resistance mechanisms against the antimicrobial agents. Emergence of resistant bacterial species has also been observed due to prolong treatment using conventional antibiotics. To combat these problems, several alternative strategies have been employed using biological and chemically synthesized compounds as antibacterial agents. Marine organisms considered as one of the potential sources for the isolation of bioactive compounds due to the easily available, cost-effective, and eco-friendly. Methods: The online search methodology was adapted for the collection of information related to the antimicrobial properties of marine-derived compounds. These compound has been isolated and purified by different purification techniques, and their structure also characterized. Furthermore, the antibacterial activities have been reported by using broth microdilution as well as disc diffusion assays. Results: The present review paper describes the antimicrobial effect of diverse secondary metabolites which are isolated and purified from the different marine organisms. The structural elucidation of each secondary metabolite has also been done in the present paper, which will help for the in silico designing of the novel and potent antimicrobial compounds. Conclusion: A thorough literature search has been made and summarizes the list of antimicrobial compounds that are isolated from both prokaryotic and eukaryotic marine organisms. The information obtained from the present paper will be helpful for the application of marine compounds as antimicrobial agents against different antibiotic-resistant human pathogenic bacteria.

Chalcones: As potent α-amylase enzyme inhibitors; synthesis, in vitro, and in silico studies

2020 ◽  
Vol 16 ◽  
Author(s):  
Mahboob Ali ◽  
Momin Khan ◽  
Khair Zaman ◽  
Abdul Wadood ◽  
Maryam Iqbal ◽  
...  
Keyword(s):  
In Silico ◽  
Enzyme Inhibitors ◽  
Biological Activities ◽  
Condensation Reaction ◽  
Type Ii Diabetes Mellitus ◽  
Spectroscopic Techniques ◽  
Chalcone Derivatives ◽  
In Silico Studies ◽  
Wide Range

: Background: The inhibition of α-amylase enzyme is one of the best therapeutic approach for the management of type II diabetes mellitus. Chalcone possesses a wide range of biological activities. Objective: In the current study chalcone derivatives (1-17) were synthesized and evaluated their inhibitory potential against α-amylase enzyme. Method: For that purpose, a library of substituted (E)-1-(naphthalene-2-yl)-3-phenylprop-2-en-1-ones was synthesized by ClaisenSchmidt condensation reaction of 2-acetonaphthanone and substituted aryl benzaldehyde in the presence of base and characterized via different spectroscopic techniques such as EI-MS, HREI-MS, 1H-, and 13C-NMR. Results: Sixteen synthetic chalcones were evaluated for in vitro porcine pancreatic α-amylase inhibition. All the chalcones demonstrated good inhibitory activities in the range of IC50 = 1.25 ± 1.05 to 2.40 ± 0.09 μM as compared to the standard commercial drug acarbose (IC50 = 1.34 ± 0.3 μM). Conclusion: Chalcone derivatives (1-17) were synthesized, characterized, and evaluated for their α-amylase inhibition. SAR revealed that electron donating groups in the phenyl ring have more influence on enzyme inhibition. However, to insight the participation of different substituents in the chalcones on the binding interactions with the α-amylase enzyme, in silico (computer simulation) molecular modeling analyses were carried out.

scholarly journals First reported quantitative microbiota in different livestock manures used as organic fertilizers in the Northeast of Thailand

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Lampet Wongsaroj ◽  
Ratmanee Chanabun ◽  
Naruemon Tunsakul ◽  
Pinidphon Prombutara ◽  
Somsak Panha ◽  
...  
Keyword(s):  
Pathogenic Bacteria ◽  
Organic Fertilizer ◽  
The Other ◽  
Organic Fertilizers ◽  
Rrna Gene ◽  
Bacterial Composition ◽  
Physiochemical Properties ◽  
Nutrient Profiles ◽  
Soil Recovery ◽  
Local Farmers

AbstractNortheastern Thailand relies on agriculture as a major economic activity, and has used high levels of agrochemicals due to low facility, and salty sandy soil. To support soil recovery and sustainable agriculture, local farmers have used organic fertilizers from farmed animal feces. However, knowledge about these animal fecal manures remains minimal restricting their optimal use. Specifically, while bacteria are important for soil and plant growth, an abundance and a diversity of bacterial composition in these animal fecal manures have not been reported to allow selection and adjustment for a more effective organic fertilizer. This study thereby utilized metagenomics combined with 16S rRNA gene quantitative PCR (qPCR) and sequencing to analyze quantitative microbiota profiles in association with nutrients (N, P, K), organic matters, and the other physiochemical properties, of the commonly used earthworm manure and other manures from livestock animals (including breed and feeding diet variations) in the region. Unlike the other manures, the earthworm manure demonstrated more favorable nutrient profiles and physiochemical properties for forming fertile soil. Despite low total microbial biomass, the microbiota were enriched with maximal OTUs and Chao richness, and no plant pathogenic bacteria were found based on the VFDB database. The microbial metabolic potentials supported functions to promote crop growth, such as C, N and P cyclings, xenobiotic degradation, and synthesis of bioactive compounds. Pearson’s correlation analyses indicated that the quantitative microbiota of the earthworm manure were clustered in the same direction as N, and conductivity, salinity, and water content were essential to control the microbiota of animal manures.

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