Antimicrobial Activity Studies Research Articles

An Expedient Three-component Synthesis of Novel Pyrido-pyrimidine Derivatives: Antimicrobial Activity, Molecular Docking, and ADME Studies

A facile and efficient protocol for one-pot three-component synthesis of a series of novel 4-substituted-2-thioxo-3,4-dihydro-1H-pyrido[1,2-a]pyrimido[4,5-d]pyrimidin-5(2H)-one derivatives has been developed. Compounds were synthesized by the reaction of 2H-pyrido[1,2-a]pyrimidine-2,4(3H)-dione, various aromatic aldehydes, and thiourea using Iodine as catalyst in acidic medium. The synthesized compounds obtained in good to excellent yields (52–83%) with improved reaction time and chloro substituent at four-position yielded the product in excellent quantity (83%). The synthesized compounds have been characterized by 1H, and 13C NMR, IR, and mass spectral analysis, and screened for their in vitro antibacterial activity against Bacillus subtilis, Salmonella typhemurium, Escherichia. coli, and Staphylococcus aureus using disk diffusion method. Biological screening revealed that the newly synthesized compounds exhibit interesting activities against several bacterial strains. Among all the synthesized compounds, the in vitro antibacterial activity displayed by compound 6j was highest against S. typhemurium with ZOI 23.5. mm (MIC = 3.125 µg/mL). Docking studies further supported the findings, and provided for the basis of linkages in terms of conventional hydrogen bonds, and pi- bonding patterns. In nutshell, the present study thus paved the way for developing lead compounds which could be potentially used as an efficient antibacterial drug in humans after appropriate animal, and clinical trials.

Biological properties of nanomaterials (literature review)

In the article reviewed and discussed literature data on biological properties of nanomaterials. The biosafety of nanomaterials is a complex and multifaceted issue that demands a comprehensive, science-based approach. Modern environmental and economic factors should be considered in this regard. The EU’s nanotechnology policy is based on ‘an integrated, safe and responsible approach’ (Communication from the Commission to the European Parliament, the Council and the European Economic and Social Committee. Regulatory aspects of nanomaterials. SEC(2008) 2036 / COM(2008) 366 final). Based on the findings of toxicity and antimicrobial activity studies, metal nanoparticles appear to be a favorable choice as antibacterial agents in developing new disinfectants. However, further measures must be taken to ensure the safe and environmentally friendly use of metal nanoparticles (MeNPs). To achieve this, it is crucial to establish toxicity parameters for MeNPs of various compositions, sizes, and concentrations. These parameters must be compared and evaluated alongside the potential effects of MeNPs on laboratory and target animals (in vivo), as well as their antibacterial performance against microorganisms of different strains (in vitro). Thus, the investigation of possible hazards associated with the use of metal nanoparticles can be effectively achieved by analyzing the fundamental systemic characteristics of biological systems under both in vivo and in vitro conditions, taking into account various aspects such as physiological, biochemical, immunological, genetic and cytological responses that may be affected by toxic effects. The literary sources analysis and article publication were conducted under the National Research Foundation of Ukraine project No. 2021.01/0076 'Development of a novel, nanoparticle-based disinfectant for deactivation of pathogens causing emergent infectious diseases'

Design and Synthesis of Novel Phthalazine Scaffolds Linked to 1,3,4–oxadiazolyl–1,2,3–triazoles as Potent Anticancer Agents: A Computational Docking Analysis

Background and objective: A study on the chemical and biological properties of molecules simultaneously comprising various heterocycles, such as fused 1,3,4–oxadiazole and 1,2,3–triazoles, has been conducted as part of our ongoing research in the field of medicinal and organic chemistry. In the present study, novel 1,3,4-oxadiazoles and 1,2,3-triazoles incorporating a phthalazine ring have been synthesized and evaluated for their anticancer activity and docking analysis. Methods: In this study, we performed ligand–based pharmacophore modeling as a promising design strategy of substituted phthalazin–1(2H)–one–1,3,4–oxadiazole acetamides (4); 1,2,3–triazole–1,3,4–oxadiazolyl)phthalazin-1(2H)-one (5) were synthesized from key intermediate 2-((5-mercapto-1,3,4-oxadiazol-2-yl)methyl)-4-methylphthalazin-1(2H)-one 2. The prepared compounds were characterized by proton and carbon nuclear magnetic resonance spectroscopy, infrared, elemental analysis, and mass spectroscopy. Synthesized scaffolds were screened for their anticancer activity against three cell lines, MCF-7, T-47D, and MDA-MB-231, by MTT assay. The prepared ligands were docked by using the input protocols, like RCSB, AutoDock 4.2, ACD ChemSketch, Open Babel, and SwissADME. Results: The final compound 5f exhibited excellent activity (IC50 = 10.21 ± 2.2, 7.53 ± 0.1 µM) against T-47D and MCF-7 cancer cell lines, respectively, and compounds 4b and 5b showed the highest % growth of inhibition (61.25 ± 0.52, 62.48 ± 0.20 µg/mL) against T-47D and MCF-7 cell lines, which has been found to be equivalent to that reported by the standard cisplatin. The prepared ligand 5f exhibited greatest bonding with amino acids AlaX:191, MetX:193, ValX:196, ThrX:140, PheX:192, TyrX:155, AsnX:90, LysX:159, LeuX:95, and IleX:14, with a docking score of –11.53 Kcal/mol, respectively. These compounds were further evaluated for their ADMET and physicochemical properties by using SwissADME. Conclusion: Phthalazine with 1,3,4–oxadiazole substituents and 1,2,3–triazoles containing 1,3,4–oxadiazole ring displayed excellent anticancer activity; some interesting relationship has also been evidenced between the synthesised structures and their antimicrobial activity and docking studies. In light of all the above findings, it can be concluded that these molecules may serve as lead molecules for further synthetic and biological evaluation.

Characterization and study of antimicrobial activity of silver nanoparticles synthesized from Escherichia coli

Characterization and study of antimicrobial activity of silver nanoparticles synthesized from Escherichia coli

Evaluation of antibacterial activity against Burkholderia pseudomallei VTCC 70157 and cytotoxicity ofpomegranate (Punica granatum) aqueous extract

Melioidosis is a severe acute infectious disease caused by Burkholderia pseudomallei, especially high epidemiological risk factors in agricultural operations with people frequently exposed to soil or water sources containing this bacterium. In this study, the thermal and gastric stability of antimicrobial activity of aqueous extracts prepared from pomegranate (Punica granatum) against Burkholderia pseudomallei VTCC 70157 (NA23) was evaluated by agar plate diffusion, minimal inhibitory dilution (MID), and minimal bactericidal dilution (MBD) methods. Additionally, the cytotoxicity of aqueous extract to HEK293, HepG2, and HT29 cell lines was also studied. The results showed that aqueous extracts of different pomegranate parts had a high antibacterial activity with an antibacterial zone diameter in the range of 21-28 mm. MID and MBD values were under 1:256 and 1:128, respectively. At the extraction temperature of 100oC, antibacterial activities were significantly higher than those of 25 and 70oC. This study also demonstrated that the antibacterial activity of the extracts highly remained under simulated gastrointestinal conditionsexcept for the MID value of the twig extracts which was increased by two times. In addition, the extracts exhibited low cytotoxicity with the tested human cell lines, with ID50 values consistently being remarkably higher than the corresponding MID values. The study results suggest that aqueous extracts of pomegranate prepared by decoction according to traditional medicine might be effective through oral administration for the treatment of melioidosis.

In vitro study of antioxidant, antimicrobial, and anticancer activities of two selected cyanobacteria found across Odisha coast, India

In vitro study of antioxidant, antimicrobial, and anticancer activities of two selected cyanobacteria found across Odisha coast, India

Design, Synthesis and Antimicrobial Activity of 1,3-Diazine Derivatives

Background: Pyrimidines have been shown to possess numerous biological activities, such as antimicrobial, anticancer, anticonvulsant, antiviral, and anti-inflammatory. Objective: Encouraged by these data, the synthesis of 2-((1H-benzo[d]imidazol-2-yl)methylthio)-4- amino-6-phenylpyrimidine-5-carbonitrile (3a-g) was performed. Methods: 4-amino-2-mercapto-6-phenylpyrimidine-5-carbonitrile was dissolved in an aqueous sodium hydroxide solution, and to this clear solution, 2-chloromethyl-1H-benzimidazole in methanol was added, and the reaction mixture was stirred under reflux to get the desired product. The structures of the newly synthesized compounds were confirmed by their physical, chemical, and spectral data. The synthesized derivatives were screened for their in vitro antibacterial activity against Gram-positive bacteria, Staphylococcus aureus and Bacillus subtilis, and Gram-negative bacteria, Escherichia coli and Pseudomonas aeruginosa, by using ciprofloxacin as a reference standard. While, their antifungal activity was evaluated against Aspergillus niger and Candida albicans using fluconazole as a reference drug. The docking study was performed to check the interactions of target compounds (3a-g) with homo sapiens DHFR (PDB: 1S3V), bacterial (S. aureus) DHFR (PDB: 2W9T), and DHPS (PDB: 1AD4) protein. The dock score and binding interactions were recorded. Result: The antimicrobial activity study indicated compounds with chloro (3b), fluoro (3f), and bromo (3g) substituents to show good antibacterial as well as antifungal activity. The docking study revealed that the same compounds, i.e., 3b, 3f, and 3g, showed good dock score and comparable interactions compared to the reference ligand (trimethoprim/sulfadiazine), which confirmed their selectivity. Conclusion: It can be presumed that the synthesized compounds have the capability for further promotion as novel antimicrobial agents.

Continuous-Flow Synthesis, Characterization, Antimicrobial Activity, and Docking Studies of Urea Derivatives of 4-(4-Aminophenyl)-3-morpholinone

Continuous-Flow Synthesis, Characterization, Antimicrobial Activity, and Docking Studies of Urea Derivatives of 4-(4-Aminophenyl)-3-morpholinone

Synthesis, Characterization, antimicrobial activity and Computational Study of New 3-(1-methyl-2-((1E,2E)-3-phenylallylidene)hydrazinyl)-5-phenyl-4H-1,2,4-triazole with some transition metal ions

Current study generated complexes of the novel heterocyclic ligand 3-(1-methyl-2-((1E,2E)-3-phenylallylidene) hydrazinyl)-5-phenyl-4H-1,2,4-triazole with Cr(lll), Co(ll), and Cu(II). Using techniques including 1H-NMR, mass spectrometry, FT-IR, and elemental analysis, scientists could determine key characteristics of the novel ligand. As spectra, Fourier transforms infrared (FTIR), magnetic susceptibility, atomic absorption, and conductance measurements were used to describe ligand complexes in contrast. Bacteria were used in an assay to test the antibacterial activity of each novel compound (Staphylococcus and Escherichia coli). Quantum chemical simulations performed using the DFT approach at the B3LYP/6-311++G level complemented the experimental data. Using Hyperchem 8.02 and the PM3 approach, this study hasdetermined the ligand's electrostatic potential and its complexes' geometries. The electrostatic potential that reveals useful data about the location's complexity.

Design, synthesis, antimicrobial activity, DFT, and molecular docking studies of pyridine-pyrazole-based dihydro-1,3,4-oxadiazoles against various bacterial and fungal targets.

Antimicrobial resistance which is increasing at an alarming rate is a severe public health issue worldwide. Hence, the development of novel antibiotics is an urgent need as microbes have developed resistance against available antibiotics. In search of novel antimicrobial agents, a convenient route for the preparation of substituted 3-(1-phenyl-3-(p-tolyl)-1H-pyrazol-4-yl)-1-(2-phenyl-5-(pyridin-3-yl)-1,3,4-oxadiazol-3(2H)-yl)prop-2-en-1-ones (6a-6o) has been adopted by using pyridine-3-carbohydrazide and various aromatic aldehydes. The newly synthesized compounds were characterized by using various spectral techniques, for example, IR, 1 H NMR, 13 C NMR, and mass spectroscopy. Synthesized hybrids were studied for in vitro antimicrobial potency against various bacterial and fungal strains. Antibacterial results revealed that compounds 6e, 6h, 6i, 6l, and 6m were found to be most active against bacterial strains as they showed minimum inhibitory concentration(MIC) value of 62.5 μg/mL while compounds 6d, 6e, and 6h showed MIC value of 200 μg/mL against Candidaalbicans. The quantum parameters that relate to the bioavailability of the compounds were computed, followed by docking with different bacterial and fungal targets like sortase A, dihydrofolate reductase, thymidylate kinase, gyrase B, sterol 14-alpha demethylase. The experimental and computational results are in good agreement.

Study of Antimicrobial Activity of Different Part of Emblica Officianalis

Emblica Officinalis is an ethnomedicinal plant that has several medicinal claims and it hasn't been explored thoroughly. Various parts of the plant are used medicinally such as antioxidant, anti-inflammatory, analgesic and anti-pyretic etc. The study aims to explore the different qualitative, quantitative, and antifungal aspects of Phyllanthus emblica. Materials and methods: The present study was conducted to evaluate the anti-microbial activity of Phyllanthus emblica extracts against Grampositive bacteria (Staphylococcus aureus), Gram-negative bacteria (E. coli), and Fungal (Candida albicans). The agar well diffusion method was used to test the antimicrobial activity. Result & Discussion: Phyllanthus emblica extracts exhibited potent antibacterial and antifungal against all the selected bacterial and fungal species. The extracts exhibited the growth inhibitory activity in a dose-dependent manner. Also, the study reveals Phyllanthus emblica shows good antimicrobial activity. Conclusion: The Phyllanthus emblica plant extracts could be used as an antimicrobial after comprehensive in-vitro biological studies.

Synthesis, characterization, DNA interaction, antimicrobial activity, DFT analysis and molecular docking studies of copper(II) complex with triazine and neocuproine

In this paper, a new copper (II) complex with neocuproine and triazine has been synthesized and characterised. In the complex [Cu (Neocup)(Triazine)H2O](NO3)2 (where neocup=2,9-dimethyl-1;10-phenanthroline,Triazine=3-(2-pyridyl)5,6-diphenyl-1.2,4-triazine) is characterized by using UV Spectra, FT-IR, EPR, and thermal analyses. UV spectra, fluorescence spectra, and cyclic voltammetry techniques were used to determine the binding mechanism of the Cu (II) complex with calf thymus DNA (CT-DNA). The stability of the prepared Cu (II) complex has been evaluated through the highest occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital (LUMO) energy gab. In addition, the molecular docking studies were indicating the Cu (II) complex into the base pairs of CT-DNA. Furthermore, the Cu (II) complex was exposed to human liver cancer cell in vitro cytotoxicity assays, using the MTT assay, one can assess cellular metabolic activity as a sign of cell viability, proliferation, and cytotoxicity. The resultant complex shows potent cytotoxic behaviour against human cell lines (HepG2). The IC50 and R2 values of an optimized complex of Cu (II) complexes are noted as 60.81 µg/ml, 19.19 µg/ml and 0.991%, 0.789% respectively. The results revealed that copper complex [Cu(Neocup)(Triazine) H2O](NO3)2 showed high potent cytotoxicity effects against human cell line (HepG2) than [Cu(phen)(tryp)I]. The complex has been implied for antibacterial properties against the staphylococcusaureus (Gram-negative (+Ve)) and the klebsiella pneumonia, Escherichia coli (Gram-negative (-Ve)) bacterial strains and the antifungal activity against C.albicanspecies, respectively. The optimized results revealed that the Cu (II) complex exhibits excellent antibacterial and antifungal activity.

One pot synthesis of 1,3,4-oxadiazoles by Lewis acid catalyst and their study of 2D-QSAR, antimicrobial and anti-tubercular activities

In the present work, Lewis acid catalyzed reactions have been carried out between mefenamic acid, substituted aldehyde and semicarbazide in the presence of ZnCl2 to give the final compounds (E)-N-(2-(5-((substitutedene)amino)-1,3,4-oxadiazol-2-yl)phenyl)-2,3-dimethylaniline, A. The synthesized compounds have been characterized by IR, 1H NMR, 13C NMR, mass spectral studies and biologically screened for the antimicrobial, antitubercular and antimalarial activities. Among the screened molecules, the molecules A1, A3, A4, A6, A8, A9, A10 show activity against different antibacterial species. The compounds, active against different antifugal species are A3, A7, A8, A9 against C. albicans, compound A3 is active against A. niger. Whereas, compound A9 shows good antimycobacterial activity. Compound A6 having 4-hydroxybenzenesubstituent exhibits promising activity against P. falciparum antimalerial parasite.

Differential Study of Antimicrobial Activity of Vancomycin and Teicoplanin (Targocid) against Strains of Staphylococcus aureus and Streptococci sp.

The glycopeptide antibiotics vancomycin and teicoplanin (targocid) are widely used in the treatment of infections caused by gram positive bacteria. Vancomyc inhibits both transglycosylation and transpeptidation reaction during peptidoglycan assembly, targocid inhibits peptidoglycan polymerization, resulting in inhibition of bacterial cell wall synthesis and cell death. In this study twenty strains of streptococcus pyogenes and streptococcus pneumoniae and twenty five strains of staphylococcus aureus were collected from different infections. MI Cs and MBCs of vancomycin and targocid were determined against the bacterial strains, the MICs of vancomycin for the streptococcus strains were 4-8 µg /ml compared with 8-16 µg/ml for targocid and MI Cs of targocid for staphylococcus aureus were 4-16 µg/ml MBC for the same strains were 8-32 µg/ml. the conclusion of this study was that targocid was less active than vancomycin against staphylococci but equal or more active against streptococci specifically it presents excellent in vitro activity against streptococcus pneumonia strains.

Synthesis, antimicrobial activity, theoretical investigation, and electrochemical studies of cellulosic metal complexes

Synthesis, antimicrobial activity, theoretical investigation, and electrochemical studies of cellulosic metal complexes

Study of Radiotherapy Properties and Antimicrobial Activity of Glyconanoparticles (GNPs) Generated from Imidazolium Salts

AbstractCarbohydrate‐based imidazolium salts (IMSs) are structural patterns for the synthesis of pharmaceutically and biologically active substances. For this purpose, the chiral furanoside‐based imidazolium salt conjugated with a cysteamine (Cyt) linker attached gold and silver nanoparticles were prepared in this study. The biological applications of the HeLa and A549 cell lines using MTT cell proliferation method were exhibited to determine the biological evaluation of NPs conjugated with sugar based imidazolium salt. The satisfactory results obtained demonstrated that the synthesized glyconanoconjugates were radiotherapeutic agents. Moreover, this modification type within a galactose derived imidazolium salt is the first work in bioapplications, especially in radiotherapy. The antimicrobial activity of IMSs and their nanoconjugates against test pathogens was also evaluated using the disc diffusion technique.

An in-vitro study of antimicrobial activity of homoeopathic medicine pyrogenium against Escherichia coli

An in-vitro study of antimicrobial activity of homoeopathic medicine pyrogenium against Escherichia coli

Study of Antimicrobial Activity of the Rubiaceae Family: A Review

The Rubiaceae tribe is one of the largest tribes in the plant kingdom which has around 13.150 species of plants, shrubs, and trees with 611 genera, the largest in the tropics on earth. The components of chemical compounds in this tribal plant that function as antibacterials are flavonoids, saponins, tannins, and alkaloids. In compiling this review article, the technique used is to use literature studies by finding sources in the form of primary data or the form of official books, national journals, and international journals. Search data using online media with the keywords Antimicrobial, Rubiaceae. Search for the main references used in this article through trusted websites such as Pubmed, Google Scholar. Based on the results of the literature data that has been done, it can be concluded that the zone of inhibition of both have an inhibition zone of > 30 mm which is categorized as a very strong antibacterial activity.

Phytochemical analysis and biological activity of the essential oil of field mugwort: Artemisia campestris L. subsp. glutinosa from the Algerian Sahara

This work focuses on the phytochemical study and biological activity (antimicrobial) of the aerial parts of the Artemisia campestris collected from the Ahaggar National Park in southern Algeria. After extraction of the essential oil, chromatographic and biological analyzes were carried out on this species. The results show an average essential oil yield of 0.6±0.02 ml per 100 g of dry plant. Chromatographic analysis of the essential oil of Artemisia campestris subsp. glutinosa is rich in monoterpene compounds (50.47%), particularly in hydrogenated forms (40.24% of α and β-pinene) and sesquiterpenes (35.75% of Spathulenol (8.47%), β-Eudesmol (4.67%), and Carvomenthene (3.37% )... The study of antimicrobial activity revealed a remarkable antifungal activity for Candida albicans that could be exploited therapeutically.

Analysis of the bioactive components in Swietenia macrophylla leaves for their antibacterial and antioxidant capabilities

In this study, the extraction of bioactive compounds from Swietenia macrophylla leaves resulted in 50 % (v/v) acetone being the best solvent for extraction of gallic acid, total phenolic compounds, hydrolyzable tannins, and flavonoid content with maximum values of 58.769 μg/mL; 38.153 mgGAE/gdw; 10.586 mg/mL and 64.172 rutin/gdw respectively. FTIR studies indicated the presence of various compounds that have antimicrobial and antibacterial properties. Further, the study of antimicrobial activity showed that the sample acted against Gram-positive bacteria, but not Gram-negative bacteria. On conducting cyclic voltammetry and differential pulse voltammetry, CV showed an anodic peak at 0.2 V with a maximum peak current was at 212 μM; whereas DPV showed various anodic peak potentials at −0.05 V, 0.13 V, 0.23 V, and 0.65 V. TLC was used to qualitatively assess the presence of various bioactive compounds in the plant sample. This study produces bioactive chemicals that are antibacterial and antioxidant.