Synthesis of 2-acetylpyridine-N-substituted thiosemicarbazonates of copper(ii) with high antimicrobial activity against methicillin resistant S. aureus, K. pneumoniae 1 and C. albicans

2019 ◽  
Vol 43 (29) ◽  
pp. 11727-11742 ◽  
Author(s):  
Mani Kaushal ◽  
Tarlok S. Lobana ◽  
Lovedeep Nim ◽  
Ritu Bala ◽  
Daljit S. Arora ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
High Antimicrobial Activity ◽  
Methicillin Resistant

The basic interest in the present study pertains to developing metal based antimicrobial agents, as several microorganisms have built resistance to the conventional drugs.

scholarly journals Algae Polyphenolic Compounds and Modern Antibacterial Strategies: Current Achievements and Immediate Prospects

Biomedicines ◽  
2020 ◽  
Vol 8 (9) ◽  
pp. 342 ◽  
Author(s):  
Natalya N. Besednova ◽  
Boris G. Andryukov ◽  
Tatyana S. Zaporozhets ◽  
Sergey P. Kryzhanovsky ◽  
Tatyana A. Kuznetsova ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Antibacterial Properties ◽  
Structural Diversity ◽  
Polyphenolic Compounds ◽  
High Antimicrobial Activity ◽  
Functional Relationships ◽  
Treatment And Prevention ◽  
Polyfunctional Compounds

The increasing drug resistance of pathogenic microorganisms raises concern worldwide and necessitates the search for new natural compounds with antibacterial properties. Marine algae are considered a natural and attractive biotechnological source of novel antibiotics. The high antimicrobial activity of their polyphenolic compounds is a promising basis for designing innovative pharmaceuticals. They can become both a serious alternative to traditional antimicrobial agents and an effective supplement to antibiotic therapy. The present review summarizes the results of numerous studies on polyphenols from algae and the range of biological activities that determine their biomedical significance. The main focus is put on a group of the polyphenolic metabolites referred to as phlorotannins and, particularly, on their structural diversity and mechanisms of antimicrobial effects. Brown algae are an almost inexhaustible resource with a high biotechnological potential for obtaining these polyfunctional compounds. An opinion is expressed that the effectiveness of the antibacterial activity of phlorotannins depends on the methods of their extraction aimed at preserving the phenolic structure. The use of modern analytical tools opens up a broad range of opportunities for studying the metabolic pathways of phlorotannins and identifying their structural and functional relationships. The high antimicrobial activity of phlorotannins against both Gram-positive and Gram-negative bacteria provides a promising framework for creating novel drugs to be used in the treatment and prevention of infectious diseases.

scholarly journals Pharmacodynamic Functions of Synthetic Derivatives for Treatment of Methicillin-Resistant Staphylococcus aureus (MRSA) and Mycobacterium tuberculosis

2020 ◽  
Vol 11 ◽  
Author(s):  
Mojdeh Dinarvand ◽  
Malcolm P. Spain ◽  
Fatemeh Vafaee
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Mycobacterium Tuberculosis ◽  
Antimicrobial Agents ◽  
Resistant Bacteria ◽  
Synthetic Compounds ◽  
Methicillin Resistant ◽  
Chemical Structures ◽  
Time Kill

Drug resistant bacteria have emerged, so robust methods are needed to evaluate combined activities of known antibiotics as well as new synthetic compounds as novel antimicrobial agents to treatment efficacy in severe bacterial infections. Marine natural products (MNPs) have become new strong leads in the drug discovery endeavor and an effective alternative to control infections. Herein, we report the bioassay guided fractionation of marine extracts from the sponges Lendenfeldia, Ircinia, and Dysidea that led us to identify novel compounds with antimicrobial properties. Chemical synthesis of predicted compounds and their analogs has confirmed that the proposed structures may encode novel chemical structures with promising antimicrobial activity against the medically important pathogens. Several of the synthetic analogs exhibited potent and broad spectrum in vitro antibacterial activity, especially against the Methicillin-resistant Staphylococcus aureus (MRSA) (MICs to 12.5 μM), Mycobacterium tuberculosis (MICs to 0.02 μM), uropathogenic Escherichia coli (MIC o 6.2 μM), and Pseudomonas aeruginosa (MIC to 3.1 μM). Checkerboard assay (CA) and time-kill studies (TKS) experiments analyzed with the a pharmacodynamic model, have potentials for in vitro evaluation of new and existing antimicrobials. In this study, CA and TKS were used to identify the potential benefits of an antibiotic combination (i.e., synthetic compounds, vancomycin, and rifampicin) for the treatment of MRSA and M. tuberculosis infections. CA experiments indicated that the association of compounds 1a and 2a with vancomycin and compound 3 with rifampicin combination have a synergistic effect against a MRSA and M. tuberculosis infections, respectively. Furthermore, the analysis of TKS uncovered bactericidal and time-dependent properties of the synthetic compounds that may be due to variations in hydrophobicity and mechanisms of action of the molecules tested. The results of cross-referencing antimicrobial activity, and toxicity, CA, and Time-Kill experiments establish that these synthetic compounds are promising potential leads, with a favorable therapeutic index for antimicrobial drug development.

scholarly journals Novel Chimeric Lysin with High-Level Antimicrobial Activity against Methicillin-Resistant Staphylococcus aureus In Vitro andIn Vivo

2013 ◽  
Vol 58 (1) ◽  
pp. 536-542 ◽  
Author(s):  
Hang Yang ◽  
Yun Zhang ◽  
Junping Yu ◽  
Yanling Huang ◽  
Xian-En Zhang ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Catalytic Domain ◽  
Intraperitoneal Administration ◽  
Methicillin Resistant ◽  
Content Type ◽  
Cell Wall Binding

ABSTRACTThe treatment of infections caused by methicillin-resistantStaphylococcus aureus(MRSA) is a challenge worldwide. In our search for novel antimicrobial agents against MRSA, we constructed a chimeric lysin (named as ClyH) by fusing the catalytic domain of Ply187 (Pc) with the non-SH3b-like cell wall binding domain of phiNM3 lysin. Herein, the antimicrobial activity of ClyH against MRSA strainsin vitroandin vivowas studied. Our results showed that ClyH could kill all of the tested clinical isolates of MRSA with higher efficacy than lysostaphin as well as its parental enzyme. The MICs of ClyH against clinicalS. aureusstrains were found to be as low as 0.05 to 1.61 mg/liter. In a mouse model, a single intraperitoneal administration of ClyH protected mice from death caused by MRSA, without obvious harmful effects. The present data suggest that ClyH has the potential to be an alternative therapeutic agent for the treatment of infections caused by MRSA.

scholarly journals Antimicrobial and Biocompatible Polycaprolactone and Copper Oxide Nanoparticle Wound Dressings against Methicillin-Resistant Staphylococcus aureus

Nanomaterials ◽  
2020 ◽  
Vol 10 (9) ◽  
pp. 1692
Author(s):  
Jennifer Balcucho ◽  
Diana M. Narváez ◽  
Jinneth Lorena Castro-Mayorga
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Copper Oxide ◽  
Metallic Nanoparticles ◽  
Antimicrobial Agents ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Inhibitory Effect ◽  
Wound Dressings ◽  
Scanning Calorimetry ◽  
Methicillin Resistant

One of the major health problems linked to methicillin-resistant Staphylococcus aureus (MRSA) is severe diabetic foot ulcers (DFU), which are associated with hospital-acquired infections, lower limb amputations and emerging resistance to the current antibiotics. As an alternative, this work aims to develop a biodegradable and biocompatible material with antimicrobial capacity to prevent DFU. This was achieved by producing active polymeric films with metallic nanoparticles dispersed through a polycaprolactone (PCL) dressing. First, the antimicrobial activity of copper oxide nanoparticles (CuONPs) was tested by the microdilution method, selecting the lowest concentration that has an inhibitory effect on MRSA. Then, active PCL films were prepared and characterized in terms of their physicochemical properties, antimicrobial performance, cytotoxicity, genotoxicity and hemocompatibility. Active films had chemical and thermal properties like the ones without the antimicrobial agents, which was confirmed through FTIR, Thermogravimetric Analysis (TGA) and Differential Scanning Calorimetry (DSC) analysis. In relation to antimicrobial activity, active PCL films inhibited MRSA growth when treated with CuONPs at a concentration of 0.07% (w/w). After exposure to the active film extracts, human foreskin fibroblast cells (ATCC® SCRC1041™) (HFF-1) exhibited a cell viability average above 80% for all treatments and no DNA damage was found. Finally, PCL films with 0.07% (w/w) CuONPs proved to be hemocompatible, and none of the films evaluated had red blood cell breakage greater than 5%, being within the acceptable limits established by the International Organization for Standardization ISO 10993-4:2002.

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 3-FORMYL INDOLE BASED SCHIFF BASES

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Singh Gurvinder ◽  
Singh Prabhsimran ◽  
Dhawan R. K.
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Analysis ◽  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Fungal Strain ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Gram Negative ◽  
E Coli

In order to develop new antimicrobial agents, a series of 3-formyl indole based Schiff bases were synthesized by reacting 3-formyl indole(indole-3-carboxaldehyde) with substituted aniline taking ethanol as solvent. The reaction was carried in the presence of small amount of p-toluene sulphonic acid as catalyst.All the synthesized compounds were characterized by IR, 1H-NMR spectral analysis. All the synthesized compounds were evaluated for antimicrobial activity against two gram positive bacterial strains (B. subtilisand S. aureus) and two gram negative bacterial strains (P. aeruginosaand E. coli) and one fungal strain (C. albicans). All the synthesized compounds were found to have moderate to good antimicrobial activity. The  standard drug amoxicillin, fluconazole were used for antimicrobial activity. Among the synthesized compounds, the maximum antimicrobial activity was shown by compounds GS04, GS07, GS08 and GS10.

Disinfection of Fruits with Activated Water

2019 ◽  
Vol 10 ◽  
pp. 1864-1872
Author(s):  
Prof. Teodora P. Popova
Keyword(s):  
Antimicrobial Activity ◽  
Aqueous Solutions ◽  
Antimicrobial Properties ◽  
The Other ◽  
Gram Negative Bacteria ◽  
High Antimicrobial Activity ◽  
Gram Negative ◽  
E Coli ◽  
Number Of Microorganisms ◽  
Lower Effect

The effect of ionized aqueous solutions (anolytes and catholyte) in the processing of fruits (cherries, morellos, and strawberries) for decontamination has been tested. Freshly prepared analytes and catholyte without the addition of salts were used, as well as stored for 7 months anolytes, prepared with 0.5% NaCl and a combination of 0.5% NaCl and 0.5% Na2CO3. The anolyte prepared with a combination of 0.5% NaCl and 0.5% Na2CO3, as well as the anolyte obtained with 0.5% NaCl, exhibit high antimicrobial activity against the surface microflora of strawberries, cherries, and sour cherries. They inactivate E. coli for 15 minutes. The other species of the fam. Enterobacteriaceae were also affected to the maximum extent, as is the total number of microorganisms, especially in cherries and sour cherries. Even stored for 7 months, they largely retain their antimicrobial properties. Anolyte and catholyte, obtained without the addition of salts, showed a lower effect on the total number of microorganisms, but had a significant effect on Gram-negative bacteria, and especially with regard to the sanitary indicative E. coli.

Assessment of Antimicrobial Activity and total Polyphenol Content of Rosa multiflora and Rosa wichuraiana

2019 ◽  
Vol 10 (04) ◽  
pp. 646-650
Author(s):  
Hyeusoo Kim ◽  
Kyeong Won Yun
Keyword(s):  
Antimicrobial Activity ◽  
Ethyl Acetate ◽  
Antimicrobial Agents ◽  
Ethyl Acetate Fraction ◽  
Rosa Multiflora ◽  
Polyphenol Content ◽  
Total Polyphenol ◽  
Water Fraction ◽  
Total Polyphenol Content ◽  
Rosa Species

The fruit of Rosa multiflora has been used as traditional herbal medicine in Asian countries. The present investigation was undertaken to study the antimicrobial activity and total polyphenol content of hexane, ether, ethyl acetate, water fraction of methanol extract of fruit and flower from Rosa multiflora and Rosa wichuraiana. Antimicrobial activity of the mentioned fractions against 3 gram-positive and 4 gram-negative bacteria using disk diffussion method. The measurement of minimal inhibition concentration (MIC) showed that the ethyl acetate fraction of the two Rosa species is the most effective against the tested bacteria. The total polyphenol content of ethyl acetate fraction of the two Rosa species is higher than the other fractions. The results indicate the antimicrobial activity was related with the total polyphenol content and the fruit and flower of the two Rosa species can be considered as a natural source of antimicrobial agents.

The Chemistry Of Antibiofilm Phytocompounds.

2020 ◽  
Vol 20 ◽  
Author(s):  
Dibyajit Lahiri ◽  
Moupriya Nag ◽  
Sayantani Garai ◽  
Rina Rani Ray
Keyword(s):  
Antimicrobial Activity ◽  
Antibiotic Resistance ◽  
Antibiotic Therapy ◽  
Antimicrobial Agents ◽  
Chemical Nature ◽  
Rapid Development ◽  
Wide Spread ◽  
Chronic Infections ◽  
Therapeutic Uses

: Phytocompounds are long known for their therapeutic uses due to their competence as antimicrobial agents. The antimicrobial activity of these bioactive compounds manifests their ability as an antibiofilm agent and is thereby proved to be competent to treat the wide spread of biofilm-associated chronic infections. Rapid development of antibiotic resistance in bacteria has made the treatment of these infections almost impossible by conventional antibiotic therapy, which forced in the switch over to the use of phytocompounds. The present overview deals with the classification of the huge array of phytocompounds according to their chemical nature, detection of their target pathogen, and elucidation of their mode of action.

Copper-catalyzed Convenient Synthesis and SAR Studies of Substituted-1,2,3-triazole as Antimicrobial Agents

2018 ◽  
Vol 16 (1) ◽  
pp. 3-10
Author(s):  
Aniket P. Sarkate ◽  
Kshipra S. Karnik ◽  
Pravin S. Wakte ◽  
Ajinkya P. Sarkate ◽  
Ashwini V. Izankar ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Cycloaddition Reaction ◽  
Dipolar Cycloaddition ◽  
One Pot ◽  
Triazole Derivatives ◽  
Sar Studies ◽  
Convenient Synthesis ◽  
Antibacterial And Antifungal

Background:A novel copper-catalyzed synthesis of substituted-1,2,3-triazole derivatives has been developed and performed by Huisgen 1,3-dipolar cycloaddition reaction of azides with alkynes. The reaction is one-pot multicomponent.Objective:We state the advancement and execution of a methodology allowing for the synthesis of some new substituted 1,2,3-triazole analogues with antimicrobial activity.Methods:A series of triazole derivatives was synthesized by Huisgen 1,3-dipolar cycloaddition reaction of azides with alkynes. The structures of the synthesized compounds were elucidated and confirmed by 1H NMR, IR, MS and elemental analysis. All the synthesized compounds were tested for their antimicrobial activity against a series of strains of Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and against the strains of Candida albicans, Aspergillus flavus and Aspergillus nigar for antifungal activity, respectively.Results and Conclusion:From the antimicrobial data, it was observed that all the newly synthesized compounds showed good to moderate level of antibacterial and antifungal activity.

Sign in / Sign up

Export Citation Format

Share Document