The prediction of the spectrum of biological activity and antimicrobial properties of diaminoazoles

2019 ◽  
Vol 65 (2) ◽  
pp. 99-102 ◽  
Author(s):  
Yu.V. Butina ◽  
T.V. Kudayarova ◽  
E.A. Danilova ◽  
M.K. Islyaikin
Keyword(s):  
Antibacterial Activity ◽  
Biological Activity ◽  
Antimicrobial Properties ◽  
Biological Properties ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Wide Range ◽  
Alternative Drugs

The work is devoted to predicting and studying biological properties of N-substituted analogs of 3,5-diamino-1,2,4-thiadiazole, which, in their turn, include in the composition of many drugs that exhibit a wide range of pharmacological actions. For searching of new alternative drugs with an antibacterial activity, but lacking resistance of microorganism strains to them, a computer screening of 2N-alkyl-substituted 5-amino-3-imino-1,2,4-thiadiazolines previously synthesized by us was carried out. The prediction of the spectrum of biological activity, as well as the determination of the probable toxicity of these compounds, was performed using the freely available computer programs PASS, Anti-Bac-Pred, and GUSAR. The study of the antibacterial activity in vitro against gram-positive (Staphylococcus aureus, Staphylococcus saprophyticus, Staphylococcus epidermidis) and gram-negative (Escherichia coli, Pseudomonas aeruginosae) bacterial strains was performed by the disco-diffusion method. Experimental data roughly correspond to the predictions.

Modifications of Isoalantolactone Leading to Effective Antibacterial and Antiviral Compounds

2020 ◽  
Vol 17 ◽  
Author(s):  
Sergey S. Patrushev ◽  
Lyubov G. Burova ◽  
Anna A. Shtro ◽  
Tatyana V. Rybalova ◽  
Dmitry S. Baev ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antiviral Activity ◽  
Influenza A ◽  
Antimicrobial Agents ◽  
Sesquiterpene Lactones ◽  
Biological Properties ◽  
Bacterial Strains ◽  
E Coli ◽  
Wide Range

Background: Natural sesquiterpene lactones are an important class of heterocyclic compounds in drug discovery since they are possessed a wide range of biological properties including antibacterial activity. Objective: The objective of this study was to synthesize of isoalantolactone derivatives with a furo[2,3-d]pyrimidin-2-оne moiety and to evaluate their antibacterial and antiviral activity. Methods: The Sonogashira cross-coupling and subsequent Ag-catalyzed cyclization reactions were the main routes of synthesis. The antibacterial activity and the ability to inhibit biofilms formation on E. coli, S. aureus, A. viscosus, P. aeruginosa and E. faecalis bacterial strains were evaluated. A study of the molecular interactions of new compounds with the multiple virulence factor regulators was performed using docking simulations. The antiviral activity against influenza A virus and human orthopneumovirus H-2А was also studied. Results: The in vitro antibacterial activity for 4 (MIC = 58.33±4.41 μg/mL) concerning E. coli and 5 (MIC = 96.5±3.25 μg/mL) against A. viscosus and the inhibition of biofilm formation for compounds 2, 4, and 5 on E. coli, S. aureus, P. aeruginosa and E. faecalis bacterial strains has been of interest for the search of improved antimicrobial agents. Compound 3 was endowed with antiviral activity to human orthopneumovirus H-2А with SI >33. The activity of the new type of hybrid compounds is depended on the substituent in the 6th position of furo[2,3-d]pyrimidin-2-one fragment. Conclusion: The decoration of isoalantolactone with a furo[2,3-d]pyrimidin-2-one fragment led to perspective antiviral and antimicrobial agents. Due to antimicrobial activity, pyridine-4-yl substituted isoalantolactone-furopyrimidinone hybrid is considered as a candidate compound to participate in further research.

scholarly journals Antibacterial Activity of Bees Gut Lactobacilli against Paenibacillus Larvae In Vitro

2018 ◽  
Vol 2 (1) ◽  
pp. 7-10 ◽  
Author(s):  
Miroslava Kačániová ◽  
Jaroslav Gasper ◽  
Margarita Terentjeva ◽  
Simona Kunová ◽  
Maciej Kluz ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antimicrobial Activities ◽  
Paenibacillus Larvae ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
De Man ◽  
Lactobacillus Spp

Abstract The aim of this study was to evaluate antimicrobial activity of bees gastrointestinal Lactobacillus spp. of against Paenibacillus larvae. Content of the intestinal tract was cultured for isolation of Lactobacillus spp. Gut homogenates were plated on de Man, Rogosa and Sharpe agar (MRS, Oxoid) plates and incubated for 48-72h at 30°C anaerobically. Then, the identification of isolates with MALDI-TOF MS Biotyper was done. The bacterial strains Lactobacillus gasseri, L. amylovorus, L. kunkeei, L. fructivorans, Paenibacillus larvae were isolated from gut content of bees. The disc diffusion method was used for the determination of antimicrobial activities of the Lactobacillus supernatant against two strains of Paenibacillus larvae. The best antimicrobial activity of Lactobacillus against Paenibacillus larvae from gut was found in L. gasseri supernatant. Lesser degree of antimicrobial activity against P. larvae was found in L. kunkeei supernatant. The strongest antibacterial activity against P. larvae CCM 4438 was found in L. gasseri and L. amylovorus and the least antibacterial activity was found in L. fructivorans.

scholarly journals An In Vitro Study on the Antimicrobial Properties of Essential Oil Modified Resin Composite against Oral Pathogens

Materials ◽  
2020 ◽  
Vol 13 (19) ◽  
pp. 4383
Author(s):  
Barbara Lapinska ◽  
Aleksandra Szram ◽  
Beata Zarzycka ◽  
Janina Grzegorczyk ◽  
Louis Hardan ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Resin Composite ◽  
Antimicrobial Properties ◽  
In Vitro Study ◽  
Diffusion Method ◽  
Oral Pathogens

Modifying the composition of dental restorative materials with antimicrobial agents might induce their antibacterial potential against cariogenic bacteria, e.g., S.mutans and L.acidophilus, as well as antifungal effect on C.albicans that are major oral pathogens. Essential oils (EOs) are widely known for antimicrobial activity and are successfully used in dental industry. The study aimed at evaluating antibacterial and antifungal activity of EOs and composite resin material (CR) modified with EO against oral pathogens. Ten EOs (i.e., anise, cinnamon, citronella, clove, geranium, lavender, limette, mint, rosemary thyme) were tested using agar diffusion method. Cinnamon and thyme EOs showed significantly highest antibacterial activity against S.mutans and L.acidophilus among all tested EOs. Anise and limette EOs showed no antibacterial activity against S.mutans. All tested EOs exhibited antifungal activity against C.albicans, whereas cinnamon EO showed significantly highest and limette EO significantly lowest activity. Next, 1, 2 or 5 µL of cinnamon EO was introduced into 2 g of CR and microbiologically tested. The modified CR showed higher antimicrobial activity in comparison to unmodified one. CR containing 2 µL of EO showed the best antimicrobial properties against S.mutans and C.albicans, while CR modified with 1 µL of EO showed the best antimicrobial properties against L.acidophilus.

scholarly journals Microwave-Hydrothermal Rapid Synthesis of Cellulose/Ag Nanocomposites and Their Antibacterial Activity

Nanomaterials ◽  
2018 ◽  
Vol 8 (12) ◽  
pp. 978 ◽  
Author(s):  
Lian-Hua Fu ◽  
Qing-Long Gao ◽  
Chao Qi ◽  
Ming-Guo Ma ◽  
Jun-Feng Li
Keyword(s):  
Antibacterial Activity ◽  
Antimicrobial Properties ◽  
Silver Ions ◽  
Heating Time ◽  
Diffusion Method ◽  
Dilution Method ◽  
Agar Dilution Method ◽  
Human Beings ◽  
Microwave Hydrothermal ◽  
Wide Range

Silver-based antimicrobial nanomaterials are considered as the most promising antibacterial agents owing to their outstanding antimicrobial efficacy and their relatively low toxicity to human beings. In this work, we report on a facile and environment-friendly microwave-hydrothermal method to prepare cellulose/Ag nanocomposites using hemicellulose as the reductant. The influences of the microwave-hydrothermal heating time and temperature, as well as the hemicellulose concentration on the formation of cellulose nanocomposites, were investigated in detail. Experimental results indicated that the hemicellulose was an effective reductant for silver ions, with higher temperature and longer heating time favoring the formation of silver with higher crystallinity and mass content in the nanocomposites. Moreover, the antimicrobial properties of the as-prepared cellulose/Ag nanocomposites were explored using Gram-positive S. aureus ATCC 6538 and Gram-negative E. coli HB 101 by both disc diffusion method and agar dilution method, and the nanocomposites showed excellent antibacterial activity. These results demonstrate that the as-prepared cellulose/Ag nanocomposites, as a kind of antibacterial material, are promising for applications in a wide range of biomedical fields.

scholarly journals The PHYTOCHEMICALS, ANTIOXIDANT AND ANTIMICROBIAL PROPERTIES OF Senna alata AND Senna tora LEAF EXTRACTS AGAINST BACTERIAL STRAINS CAUSING SKIN INFECTIONS

2019 ◽  
Vol 2 (1) ◽  
pp. 19
Author(s):  
Murni Halim
Keyword(s):  
Leaf Extract ◽  
Antimicrobial Properties ◽  
Inhibition Zone ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Leaf Extracts ◽  
Natural Drugs ◽  
Senna Alata

A study was carried out to screen for phytochemical constituents and assess the antioxidant and antimicrobial activities of Senna alata and Senna tora leaf extracts. The leaves were first dried at room temperature and 50°C in an oven prior to solvent extraction using ethanol and methanol. The in-vitro qualitative assays showed that both S. alata and S. tora leaf extracts contained bioactive and secondary metabolites components such as tannins, steroids, saponin, terpenoids, glycosides, flavonoids and phenols. The antioxidant activity and capacity test were carried out by conducting free radical of 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity and Ferric reduction antioxidant plasma (FRAP) assays. Both assays showed S. tora leaf extract has higher antioxidant capacity than S. alata leaf extract. The efficacy of these leaf extracts were tested against skin pathogens through agar well diffusion method. S. alata extract showed an inhibition zone (1.15 – 1.59 mm) against Pseudomonas aeruginosa while S. tora extracts exhibited a strong antimicrobial activity against S. epidermidis (inhibition zone of 12 – 16.94 mm) followed by P. aeruginosa (inhibition zone of 1 – 1.59 mm). Nonetheless, no inhibition zone was observed for S. aureus by both leaf extracts. The phytochemicals and antioxidant constituents as well as inhibitory potential on skin pathogens possessed by S. alata and S. tora leave highlighted their potential utilization in the development of natural drugs or cosmetics to treat skin related diseases or infections.

scholarly journals Essential Oil from Origanum vulgare Completely Inhibits the Growth of Multidrug-Resistant Cystic Fibrosis Pathogens

2016 ◽  
Vol 11 (6) ◽  
pp. 1934578X1601100 ◽  
Author(s):  
Giovanna Pesavento ◽  
Valentina Maggini ◽  
Isabel Maida ◽  
Antonella Lo Nostro ◽  
Carmela Calonico ◽  
...  
Keyword(s):  
Cystic Fibrosis ◽  
Essential Oil ◽  
Multidrug Resistant ◽  
Diffusion Method ◽  
Achromobacter Xylosoxidans ◽  
Bacterial Strains ◽  
Origanum Vulgare ◽  
Disk Diffusion Method ◽  
Wide Range

Essential oils (EOs) are known to inhibit the growth of a wide range of microorganisms. Particularly interesting is the possible use of EOs to treat multidrug-resistant cystic fibrosis (CF) pathogens. We tested the essential oil (EO) from Origanum vulgare for in vitro antimicrobial activity, against three of the major human opportunistic pathogens responsible for respiratory infections in CF patients; these are methicillin-resistant Staphylococcus aureus, Stenotrophomonas maltophilia and Achromobacter xylosoxidans. Antibiotic susceptibility of each strain was previously tested by the standard disk diffusion method. Most strains were resistant to multiple antibiotics and could be defined as multi-drug-resistant (MDR). The antibacterial activity of O. vulgare EO (OEO) against a panel of 59 bacterial strains was evaluated, with MIC and MBC determined at 24, 48 and 72 hours by a microdilution method. The OEO was effective against all tested strains, although to a different extent. The MBC and MIC of OEO for S. aureus strains were either lower or equal to 0.50%, v/v, for A. xylosoxidans strains were lower or equal to 1% and 0.50%, v/v, respectively; and for S. maltophilia strains were lower or equal to 0.25%, v/v. The results from this study suggest that OEO might exert a role as an antimicrobial in the treatment of CF infections.

scholarly journals Antibacterial Activity and Essential Oil Composition of Satureja spicigera from Iran

2009 ◽  
Vol 64 (1-2) ◽  
pp. 20-24 ◽  
Author(s):  
Fereshteh Eftekhar ◽  
Fereshteh Raei ◽  
Morteza Yousefzadi ◽  
Samad Nejad Ebrahimi ◽  
Javad Hadian
Keyword(s):  
Antibacterial Activity ◽  
Essential Oil ◽  
Essential Oil Composition ◽  
Diffusion Method ◽  
Resistant Organism ◽  
Disc Diffusion ◽  
Oil Composition ◽  
Bacterial Strains ◽  
Full Flowering

The aerial parts of Satureja spicigera were collected at full flowering stage at Gazvin, Iran. The essential oil was isolated by hydrodistillation and analyzed by a combination of capillary GC and GC-MS. Fourteen compounds were identified, of which carvacrol (53.74%) and thymol (36.03%) were the main constituents, representing 99.12% of the total oil. The in vitro antibacterial activity of the essential oil was determined against six ATCC standard bacterial strains (Bacillus subtilis, Enterococcus faecalis, Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa) using disc diffusion as well as measurement of minimum inhibitory concentrations. The disc diffusion results and MIC values indicated high inhibitory activity against the test bacteria. The most susceptible organisms were the Gram-positive B. subtilis and S. aureus followed by E. faecalis, usually resistant to most common antibiotics. Among the Gram-negative bacteria, E. coli and K. pneumoniae were highly sensitive to the different oil concentrations in the disc diffusion method. Finally, P. aeruginosa, a highly resistant organism to most antibiotics, showed moderate susceptibility to Satureja spicigera essential oil.

scholarly journals Synthesis, Characterization, and Biologic Activity of New Acyl Hydrazides and 1,3,4-Oxadiazole Derivatives

Molecules ◽  
2020 ◽  
Vol 25 (14) ◽  
pp. 3308
Author(s):  
Irina Zarafu ◽  
Lilia Matei ◽  
Coralia Bleotu ◽  
Petre Ionita ◽  
Arnaud Tatibouët ◽  
...  
Keyword(s):  
Gene Expression ◽  
Cell Cycle ◽  
Antibacterial Activity ◽  
Drug Metabolism ◽  
Biological Properties ◽  
Bacterial Strains ◽  
New Information ◽  
Diffusion Technique ◽  
Phase Compound

Starting from isoniazid and carboxylic acids as precursors, thirteen new hydrazides and 1,3,4-oxadiazoles of 2-(4-substituted-phenoxymethyl)-benzoic acids were synthesized and characterized by appropriate means. Their biological properties were evaluated in terms of apoptosis, cell cycle blocking, and drug metabolism gene expression on HCT-8 and HT-29 cell lines. In vitro antimicrobial tests were performed by the microplate Alamar Blue assay for the anti-mycobacterial activities and an adapted agar disk diffusion technique for other non-tubercular bacterial strains. The best antibacterial activity (anti-Mycobacterium tuberculosis effects) was proved by 9. Compounds 7, 8, and 9 determined blocking of G1 phase. Compound 7 proved to be toxic, inducing apoptosis in 54% of cells after 72 h, an effect that can be predicted by the increased expression of mRNA caspases 3 and 7 after 24 h. The influence of compounds on gene expression of enzymes implicated in drug metabolism indicates that synthesized compounds could be metabolized via other pathways than NAT2, spanning adverse effects of isoniazid. Compound 9 had the best antibacterial activity, being used as a disinfectant agent. Compounds 7, 8, and 9, seemed to have antitumor potential. Further studies on the action mechanism of these compounds on the cell cycle may bring new information regarding their biological activity.

scholarly journals In vitro antibacterial activity of Terminalia chebula leaf gall extracts against some human pathogenic strains

2012 ◽  
Vol 1 (8) ◽  
pp. 217-220 ◽  
Author(s):  
BE Ravi Shankara ◽  
YL Ramachandra ◽  
S Sundara Rajan ◽  
J Preetham ◽  
PS Sujan Ganapathy
Keyword(s):  
Antibacterial Activity ◽  
Aqueous Extract ◽  
Ethanol Extract ◽  
Pharmaceutical Journal ◽  
Inhibitory Effect ◽  
Diffusion Method ◽  
Terminalia Chebula ◽  
Bacterial Strains ◽  
South Indian

The leaf galls of Terminalia chebula is used widely as Karkatasringi in south Indian markets. Karkatashringi is an important crude drug employed in various indigenous systems of medicine against several diseases and the drug has diverse medicinal properties. The present study was carried out to understand the antimicrobial activity of various extracts. The antibacterial activity of T. chebula (leaf gall) was evaluated against ten bacterial strains including Gram-positive and Gram-negative bacteria using the agar-well diffusion method. Among the two extracts tested, the ethanol extract presented the best results against all the bacteria while aqueous extract showed moderate inhibition of the microbial growth. Each extract is unique against different microorganisms; Staphylococcus aureus was more susceptible to both extract among the tested organisms, whereas Serratia marcescens and Proteus mirabilis were less susceptible for ethanol and aqueous extract respectively. The inhibitory effect of the extracts was compared with standard antibiotic Ciprofloxacin.DOI: http://dx.doi.org/10.3329/icpj.v1i8.11254 International Current Pharmaceutical Journal 2012, 1(8): 217-220 

scholarly journals FORMULATION, CHARACTERIZATION AND DETERMINATION OF ANTIBACTERIAL ACTIVITY OF POMEGRANATE (Punicagranatum) GEL.

2015 ◽  
Vol 7 ◽  
pp. 13
Author(s):  
Afendi Dahlan ◽  
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antimicrobial Properties ◽  
Pathogenic Microorganisms ◽  
Wide Range ◽  
Common Skin

revious studies have shown that Punicagranatum (P. granatum) extract exhibited antimicrobial activity against a wide range of pathogenic microorganisms. Thus, the aim of study was to formulate and determine the effectiveness of antimicrobial properties of gel containing P. granatummethanol extract against selected common skin pathogens including Staphylococcus aureus, Staphylococcusepidermidis, Pseudomonas aeruginosaand Candidaalbicans.

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