scholarly journals Synthesis and Antibacterial Activity of New Spiro[thiadiazoline-(pyrazolo[3,4-d]pyrimidine)] Derivatives

2015 ◽  
Vol 2015 ◽  
pp. 1-6 ◽  
Author(s):  
Mohammed El Fal ◽  
Youssef Ramli ◽  
Abdelfettah Zerzouf ◽  
Ahmed Talbaoui ◽  
Youssef Bakri ◽  
...  

New heterocyclic compounds spiroderivatives of allopurinol of biological interest were prepared from allopurinol via thionation and 1,3-dipolar cycloaddition and were produced in high to excellent yields. These compounds were characterized on the basis of spectral and spectroscopic data (1H NMR,13C, IR, and MS). The antibacterial activity of the synthesized products was studied using bacterial strains:Staphylococcus aureus,Enterococcus faecalis,Escherichia coli, andPseudomonas aeruginosa. Compounds having an ethyl group showed the best activity with MIC value of 31.25 µg/mL againstStaphylococcus aureusandStreptococcus fasciens.

2008 ◽  
Vol 3 (1) ◽  
pp. 1934578X0800300 ◽  
Author(s):  
Musa Chacha ◽  
Renameditswe Mapitse ◽  
Anthony J. Afolayan ◽  
Runner R. T. Majinda

Investigation of the roots of Ceriops tagal led to the isolation of a new isopimarane, together with the known diterpenes isopimar-8(14)-en-15,16-diol and erythroxyl-4(17),15(16)-dien-3-one. The structure of the new compound was identified as isopimar-8(14)-en-16-hydroxy-15-one. These structures were determined from extensive spectroscopic data analysis. The isolates were screened for antibacterial activity using the agar dilution method against ten test bacterial strains ( Bacillus cereus, Escherichia coli, Klebsiella pneumoniae, Micrococcus kristinae, Pseudomonas aeruginosa, Salmonella pooni, Serratia marcescens, Staphylococcus aureus, S. epidermidis and Streptococcus pyrogens). Isopimar-8(14)-en-16-hydroxy-15-one exhibited activity, with MIC values of 0.5 mg/mL against Streptococcus pyrogens; 0.25 mg/mL against Salmonella pooni and 0.1 mg/mL against Bacillus cereus, Staphylococcus aureus and Micrococcus kristinae.


Marine Drugs ◽  
2019 ◽  
Vol 17 (8) ◽  
pp. 433 ◽  
Author(s):  
Meng Bai ◽  
Guo-Lei Huang ◽  
Rong-Qing Mei ◽  
Bin Wang ◽  
You-Ping Luo ◽  
...  

Three new lactones penicilactones A−C (1−3) were obtained from the mangrove-derived fungus Penicillium sp. TGM112. Their structures and absolute configurations were determined by detailed NMR, MS spectroscopic data, Mo2(OAc)4-induced electronic circular dichroism (ECD), and circular dichroism (CD) spectroscopy. Compound 1 showed antibacterial activity against Staphylococcus aureus with an MIC value of 6.25 μg/mL. Compound 2 showed insecticidal activity against newly hatched larvae of Culex quinquefasciatus with the LC50 value of 78.5 (±0.58) μg/mL.


2006 ◽  
Vol 61 (11-12) ◽  
pp. 769-772
Author(s):  
Ali Fakhimi ◽  
Mehrdad Iranshahi ◽  
Seyed Ahmad Emami ◽  
Esam Amin-Ar-Ramimeh ◽  
Gholamreza Zarrini ◽  
...  

Abstract In this study the enhancement effect of Sophora pachy- carpa roots’ acetone extract on the antibacterial activity of gentamycin was evaluated against Staphylococcus au­reus. Disc diffusion and broth dilution methods were used to determine the antibacterial activity of gentamy­cin in the absence and presence of plant extract and its various fractions separated by TLC. A clinical isolate of S. aureus was used as test strain. The active component of the plant extract involved in enhancement of genta- mycin’s activity had Rf = 0.72 on a TLC plate. The spec­tral data (1H NMR. 13CNMR) of this compound re­vealed that this compound was 5,7,2′,4′-tetrahydroxy-8- lavandulylflavanone (sophoraflavanone G), previously isolated from Sophora exigua. In the presence of 0.03 μg/ mL of sophoraflavanone G the MIC value of gentamy­cin for S. aureus decreased from 32 to 8 μg/mL (a four­fold decrease). These results signify that the ultra-low concentration of sophoraflavanone G potentiates the an­timicrobial action of gentamycin suggesting a possible utilization of this compound in combination therapy against Staphylococcus aureus.


2006 ◽  
Vol 61 (9-10) ◽  
pp. 769-772 ◽  
Author(s):  
Ali Fakhimi ◽  
Mehrdad Iranshahi ◽  
Seyed Ahmad Emami ◽  
Esam Amin-Ar-Ramimeh ◽  
Gholamreza Zarrini ◽  
...  

AbstractIn this study the enhancement effect of Sophora pachycarpa roots’ acetone extract on the antibacterial activity of gentamycin was evaluated against Staphylococcus aureus. Disc diffusion and broth dilution methods were used to determine the antibacterial activity of gentamycin in the absence and presence of plant extract and its various fractions separated by TLC. A clinical isolate of S. aureus was used as test strain. The active component of the plant extract involved in enhancement of gentamycin’s activity had Rƒ = 0.72 on a TLC plate. The spectral data (1H NMR, 13C NMR) of this compound revealed that this compound was 5,7,2′,4′-tetrahydroxy-8- lavandulylflavanone (sophoraflavanone G), previously isolated from Sophora exigua. In the presence of 0.03 μg/ mL of sophoraflavanone G the MIC value of gentamycin for S. aureus decreased from 32 to 8 μg/mL (a fourfold decrease). These results signify that the ultra-low concentration of sophoraflavanone G potentiates the antimicrobial action of gentamycin suggesting a possible utilization of this compound in combination therapy against Staphylococcus aureus.


2020 ◽  
Vol 26 (1) ◽  
pp. 137-147
Author(s):  
Shruthi T G ◽  
Sangeetha Subramanian ◽  
Sumesh Eswaran

AbstractEmerging bacterial resistance is causing widespread problems for the treatment of various infections. Therefore, the search for antimicrobials is a never-ending task. Hydrazones and quinolines possess a wide variety of biological activities. Herewith, eleven quinoline hydrazone derivatives have been designed, synthesized, characterized and evaluated for their antibacterial activity and antitubercular potential against Mtb WT H37Rv. Compounds QH-02, QH-04 and QH-05 were found to be promising compounds with an MIC value of 4 μg/mL against Mtb WT H37Rv. Compounds QH-02, QH-04, QH-05, and QH-11 were also found to be active against bacterial strains including Acinetobacter baumanii, Escherichia coli and Staphylococcus aureus. Further, we have carried out experiments to confirm the cytotoxicity of the active compounds and found them to be non-toxic.


2021 ◽  
Vol 5 (1) ◽  
pp. 1-9
Author(s):  
Antonio Carlos Pereira de Menezes Filho ◽  
Matheus Vinícius Abadia Ventura ◽  
Carlos Frederico de Souza Castro

Tibouchina granulosa is a species that blooms annually in several regions of Brazil. This species is still little explored in terms of phytocompounds in all organs of this plant, especially the floral organ. Flowers of T. granulosa were collected in the municipality of Rio Verde, Goiás, Brazil, in 2021. The hydroethanolic floral extract was prepared by maceration and qualitative phytochemical (colorimetric reactions and salt formation) and antibacterial analyzes performed and the results expressed in millimeters of inhibition at different concentrations in mg mL-1. Several phytochemical classes were observed with positive results, especially for alkaloids, phenolics, oxylates, saponins, carbohydrates and tannins. As for the bacterial assay, potential antibacterial activity was observed for all bacterial strains tested, except for Salmonella serovar Thyphymurium and serovar Enteritidis. Expressive inhibitions were observed for Enterococcus faecalis > Pseudomonas aeruginosa > Staphylococcus aureus and Escherichia coli at the highest concentrations between 100-50 mg mL-1. The floral extract of Tibouchina granulosa showed phytotherapeutic potential with the presence of several phytochemical groups and expressive antibacterial activity.


Author(s):  
Haribhai Rabari ◽  
Hetal Vankar ◽  
Beenkumar Prajapati

The emergence of multidrug microbial resistance is the main challenges that the modern scientists have so far been facing in the recent era. In this respect, new series of drug classes having potential to give antimicrobial effect have been synthesized. A new series of 5- substituted-1,10 b-dihydroimidazole[1,2-c]quinazoline derivatives 8a-e have been synthesized and screened for antibacterial activity and antifungal activity. Synthesized derivatives were characterized by IR, MASS and 1H-NMR spectroscopy. Synthesized compounds show good activity, which was comparable to the standard drug and it can be useful for the further clinical study. Antibacterial activity was evaluated against four different pathogenic bacterial strains like Staphylococcus aureus, Enterococcus faecalis, Escherichia coli and Pseudo-monas aeruginosa. Among the screened compounds, 8e show good antibacterial activity against Staphylococcus aureus and Escherichia coli with MIC of 50 and 100 μg/ml respectively. Antifungal activity was evaluated  against two strains of fungi. Among the synthesized derivates, compound 8c was emerged out as the potent antifungal compound against Candida albicans and Aspergillus niger with MIC of 25 μg/ml and 75μg/ml respectively. Compound 8e also shows good antifungal activity with MIC of 50 μg/ml against both Candida albicans and Aspergillus niger. The overall results of this study indicated that  synthesized quinazoline derivatives had the potential to act as an antibacterial and antifungal agent, hence further investigation is warranted.


2014 ◽  
Vol 875-877 ◽  
pp. 87-90 ◽  
Author(s):  
Chutimon Satirapipathkul ◽  
Tanakan Chatdum

The film-forming potential of isolate of seed polysaccharide fromCassia fistulawas investigated. Increasing the glycerol concentration in the film increased elongation at break, film solubility and water vapor permeability but decreased tensile strength (TS). The film impregnated with the acetone extract ofAtractylodes lanceawas assessed for inhibition ofEscherichia coliandStaphylococcus aureus. The obtained results showed that the films exhibited antibacterial activity against both bacterial strains. Disc-diffusion assay revealed that the film resulted in a larger inhibition zone around the film onStaphylococcus aureusthan it did onEscherichia coliat the same extract concentrations (0.1 to 0.9 wt %). It can be seen that the film has satisfactory physical and antibacterial properties.


Molecules ◽  
2020 ◽  
Vol 25 (10) ◽  
pp. 2370 ◽  
Author(s):  
Vladimir N. Koshelev ◽  
Olga V. Primerova ◽  
Stepan V. Vorobyev ◽  
Ludmila V. Ivanova

A series of benzotriazole, cyclic amides and pyrimidine derivatives, containing 2,6-di-tert-butyl-phenol fragments, were synthesized. The redox properties of obtained compounds were studied using the cyclic voltammetry on a platinum electrode in acetonitrile. The oxidation potentials of all substances were comparable to those of BHT. The obtained compounds were tested for their antibacterial activity, and N-(2-(3,5-di-tert-butyl-4-hydroxyphenyl)-2-oxoethyl)isatin (32 μg/mL) exerted good activity against Staphylococcus aureus.


Scientifica ◽  
2020 ◽  
Vol 2020 ◽  
pp. 1-8
Author(s):  
Hasanga Rathnayake ◽  
Manikkuwadura Hasara Nethmini De Zoysa ◽  
Ruwani Punyakanthi Hewawasam ◽  
Weerasinghe Mudiyanselage Dilip Gaya Bandara Wijayaratne

Methicillin-resistant Staphylococcus aureus (MRSA) is a major cause of hospital- and community-acquired infections worldwide. Therefore, this study was conducted to explore the antibacterial activity of the two medicinal plants Epaltes divaricata and Vetiveria zizanioides against strains of MRSA which were isolated from patients with skin and soft tissue infections. Hexane, ethanol, and water extracts of E. divaricata (whole plant) and V. zizanioides (roots) were prepared. Clinical isolates of MRSA strains (n = 20) were used for the study. Bacterial susceptibility was tested using a disc diffusion assay. Minimum inhibitory concentration (MIC) was determined by a broth microdilution method. Vancomycin was used as the positive control. Hexane, ethanol, and water extracts of E. divaricata showed inhibitory zones against MRSA. Except for water extract, both hexane and ethanol extracts of V. zizanioides showed inhibitory zones. MIC ranges of hexane, ethanol, and water extracts in E. divaricata were 0.012–0.32 mg/mL, 0.019–2.4 mg/mL, and 0.019–0.48 mg/mL, respectively. Respective MIC ranges of hexane and ethanol extracts of V. zizanioides were 0.003–0.032 mg/mL and 0.019–2.4 mg/mL. The hexane extract of V. zizanioides inhibited 55% of the selected MRSA strains at a relatively low MIC value of 0.012 mg/mL. The hexane extract of both plants demonstrated inhibition of 75% of MRSA strains at a MIC value of 0.064 mg/mL. Ethanol extract of V. zizanioides and E. divaricata, respectively, inhibited 70% and 45% of MRSA strains at the MIC of 0.096 mg/mL, whereas water extract of E. divaricata inhibited 80% of MRSA strains at the same MIC. Both E. divaricata and V. zizanioides were equally effective against MRSA at a MIC of 0.064 mg/mL. But V. zizanioides was more effective since the hexane extract inhibited more than 50% of MRSA strains at significantly a lower MIC value of 0.012 mg/mL. Fractionation, purification, and identification of active compounds will warrant further evaluation of the therapeutic potential of both plant extracts.


Sign in / Sign up

Export Citation Format

Share Document