The antibacterial activity of isatin hybrids

2021 ◽  
Vol 21 ◽  
Author(s):  
Bi Liu ◽  
Dan Jiang ◽  
Guowen Hu
Keyword(s):  
Bacterial Infections ◽  
Rational Design ◽  
Synergistic Effects ◽  
Antibacterial Properties ◽  
Resistance Mechanisms ◽  
Patient Morbidity ◽  
Hybrid Molecules ◽  
Wide Range ◽  
Spectrum Activity ◽  
Broad Spectrum Activity

: Bacterial infections which cause a wide range of host immune disorders leading to local and systemic tissue damage, are still one of the main causes of patient morbidity and mortality worldwide. Treatment of bacterial infections is challenging, which is mainly attributed to the rapidly evolving resistance mechanisms, creating an urgent demand to develop novel antibacterial agents. Hybridization is one of the most promising strategies in the development of novel antibacterial drugs with the potential to address drug resistance since different pharmacophores in the hybrid molecules could modulate multiple targets and exert synergistic effects. Isatin, distributed widely in nature, can exert antibacterial properties through acting on diverse enzymes, proteins, and receptors. Accordingly, hybridization of isatin pharmacophores with other antibacterial pharmacophores in one molecule may provide novel antibacterial candidates with broad-spectrum activity against various pathogens, including drug-resistant forms. This review aims to outline the recent advances of natural and synthetic isatin hybrids with antibacterial potential and summarize the structure-activity relationship (SAR) to provide an insight for the rational design of more active candidates, covering articles published between January 2012 and June 2021.

scholarly journals Rational design, synthesis and testing of novel tricyclic topoisomerase inhibitors for the treatment of bacterial infections part 2

2020 ◽  
Vol 11 (12) ◽  
pp. 1379-1385
Author(s):  
R. Kirk ◽  
A. Ratcliffe ◽  
G. Noonan ◽  
M. Uosis-Martin ◽  
D. Lyth ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Bacterial Infections ◽  
Rational Design ◽  
Topoisomerase Ii ◽  
Topoisomerase Inhibitors ◽  
Design Synthesis ◽  
Pharmacokinetic Properties ◽  
Spectrum Activity ◽  
Broad Spectrum Activity

We disclose the discovery of REDX07965, a novel tricyclic topoisomerase inhibitor (NTTI) which has broad spectrum activity, favourable in vitro pharmacokinetic properties and selectivity versus human topoisomerase II.

scholarly journals Nanometals-Containing Polymeric Membranes for Purification Processes

Materials ◽  
2021 ◽  
Vol 14 (3) ◽  
pp. 513
Author(s):  
Anna Rabajczyk ◽  
Maria Zielecka ◽  
Krzysztof Cygańczuk ◽  
Łukasz Pastuszka ◽  
Leszek Jurecki
Keyword(s):  
Synergistic Effects ◽  
Membrane Surface ◽  
Antibacterial Properties ◽  
Polymeric Membranes ◽  
Treatment Processes ◽  
Wide Range ◽  
Different Types ◽  
Type Size ◽  
Titanium Zinc ◽  
Membrane Surface Charge

A recent trend in the field of membrane research is the incorporation of nanoparticles into polymeric membranes, which could produce synergistic effects when using different types of materials. This paper discusses the effect of the introduction of different nanometals such as silver, iron, silica, aluminum, titanium, zinc, and copper and their oxides on the permeability, selectivity, hydrophilicity, conductivity, mechanical strength, thermal stability, and antiviral and antibacterial properties of polymeric membranes. The effects of nanoparticle physicochemical properties, type, size, and concentration on a membrane’s intrinsic properties such as pore morphology, porosity, pore size, hydrophilicity/hydrophobicity, membrane surface charge, and roughness are discussed, and the performance of nanocomposite membranes in terms of flux permeation, contaminant rejection, and antifouling capability are reviewed. The wide range of nanocomposite membrane applications including desalination and removal of various contaminants in water-treatment processes are discussed.

scholarly journals Risk-benefit associated with azithromycin: A brief review

2020 ◽  
Vol 1 (2) ◽  
pp. 1-5
Author(s):  
Anil Kumar Pradhan ◽  
Ajit Nahak ◽  
Gyanendra Narayan Mohapatra
Keyword(s):  
Bacterial Infections ◽  
Respiratory Tract Infections ◽  
Hepatic Injury ◽  
Review Of Literature ◽  
Lower Respiratory Tract Infections ◽  
Sexually Transmitted ◽  
Spectrum Activity ◽  
Therapeutic Properties ◽  
Tract Infections ◽  
Broad Spectrum Activity

Introductions: Azithromycin is the most popular prescribed antimicrobial agent around the world. It comes under the class of macrolide antibiotics. Because of its higher efficacy, tolerance, and broad-spectrum activity, it is primarily used in upper and lower respiratory tract infections, some sexually transmitted infections, and major bacterial infections. Methods: Pieces of literature were reviewed to access the risk and benefits associated with azithromycin. Results: Generally, this is commercially available in solids, liquids, and ophthalmic formulations due to its minimal adverse events. It is also used in the case of COVID-19 drug therapy due to its pharmacological and therapeutic properties. Conclusions: The review of literature presented that it may increase the risk of cardiac death, hepatic injury, ototoxicity, hypersensitivity reactions.

Selenium Nanoparticles Inhibit Various Bacterial Growth on Paper Towels

2014 ◽  
Vol 1626 ◽  
Author(s):  
Qi Wang ◽  
Thomas J. Webster
Keyword(s):  
Bacterial Infections ◽  
Antibacterial Properties ◽  
Selenium Nanoparticles ◽  
Coated Paper ◽  
Selenium Nanoparticle ◽  
Wide Range ◽  
Clinical Environments ◽  
Uncoated Paper ◽  
Paper Towels

ABSTRACTBacterial infections are commonly found on paper towels and other paper products leading to the potential spread of bacteria and consequent health concerns. The objective of this in vitro study was to introduce antibacterial properties to paper towel surfaces by coating them with selenium nanoparticles. Results showed that the selenium nanoparticle coated paper towels inhibited the growth of S. Aureus and P. aeruginosa by 80%∼90% after 72 hours compared with the uncoated paper towels. Thus, the study showed that nano-selenium coated paper towels may lead to an increased eradication of bacteria to more effectively clean a wide-range of clinical environments, thus, improving health.

Combating bacterial resistance by combination of antibiotics with antimicrobial peptides

2019 ◽  
Vol 91 (2) ◽  
pp. 199-209 ◽  
Author(s):  
Dean E. Sheard ◽  
Neil M. O’Brien-Simpson ◽  
John D. Wade ◽  
Frances Separovic
Keyword(s):  
Antimicrobial Peptides ◽  
Bacterial Infections ◽  
Bacterial Resistance ◽  
Synergistic Effects ◽  
Resistance Mechanisms ◽  
Bacterial Strains ◽  
Diverse Range ◽  
Recent Emergence ◽  
Agricultural Industries ◽  
Conventional Antibiotics

Abstract The overuse of antibiotics in the healthcare and agricultural industries has led to the worldwide spread of bacterial resistance. The recent emergence of multidrug resistant (MDR) bacteria has resulted in a call for the development of novel strategies to address this global issue. Research on a diverse range of antimicrobial peptides (AMPs) has shown promising activity against several resistant strains. Increased understanding of the mode of action of AMPs has shown similarity and complementarity to conventional antibiotics and the combination of both has led to synergistic effects in some cases. Combination therapy has been widely used to combat MDR bacterial infections and the recent focus on their application with AMPs may allow antibiotics to be effective against resistant bacterial strains. By conjugation of an antibiotic onto an AMP, a compound may be produced with possibly greater activity and with reduced side-effects and toxicity. The AMP in these conjugates may also act as a unique adjuvant for the antibiotic by disrupting the resistance mechanisms used by bacteria thus allowing the antibiotic to once again be effective. This mini-review outlines some of the current and past work in combining AMPs with conventional antibiotics as strategies to address bacterial resistance.

scholarly journals Chitosan Oligosaccharides Coupling Inhibits Bacterial Biofilm-Related Antibiotic Resistance against Florfenicol

Molecules ◽  
2020 ◽  
Vol 25 (24) ◽  
pp. 6043
Author(s):  
Xianghua Yuan ◽  
Jing Liu ◽  
Ruilian Li ◽  
Junlin Zhou ◽  
Jinhua Wei ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Bacterial Infections ◽  
Bacterial Biofilm ◽  
Bacterial Biofilms ◽  
Gram Negative Bacteria ◽  
Planktonic Cells ◽  
Gram Negative ◽  
Chitosan Oligosaccharides ◽  
Spectrum Activity ◽  
Broad Spectrum Activity

The formation of bacterial biofilms has increased the resistance of bacteria to various environmental factors and is tightly associated with many persistent and chronic bacterial infections. Herein we design a strategy conjugating florfenicol, an antibiotic commonly used in the treatment of streptococcus, with the antimicrobial biomaterial, chitosan oligosaccharides. The results demonstrated that the florfenicol-COS conjugate (F-COS) efficiently eradicated the mature Streptococcus hyovaginalis biofilm, apparently inhibiting drug resistance to florfenicol. A quantity of 250 μg/mL F-COS showed effective inhibitory activity against planktonic cells and biofilm of the bacteria, and a 4-fold improvement of the F-COS compared to unmodified florfenicol was observed. Furthermore, the conjugate showed a broad-spectrum activity against both Gram-positive and Gram-negative bacteria. It suggested that F-COS might have a potential for application in the treatment of biofilm-related infections.

scholarly journals Antibacterial Properties of Organosulfur Compounds of Garlic (Allium sativum)

2021 ◽  
Vol 12 ◽  
Author(s):  
Sushma Bagde Bhatwalkar ◽  
Rajesh Mondal ◽  
Suresh Babu Naidu Krishna ◽  
Jamila Khatoon Adam ◽  
Patrick Govender ◽  
...  
Keyword(s):  
Bacterial Infections ◽  
Allium Sativum ◽  
New Technologies ◽  
Antibacterial Properties ◽  
World Health ◽  
Health Concern ◽  
Organosulfur Compounds ◽  
Wide Range ◽  
The World ◽  
Novel Antibiotics

Garlic (Allium sativum), a popular food spice and flavoring agent, has also been used traditionally to treat various ailments especially bacterial infections for centuries in various cultures around the world. The principal phytochemicals that exhibit antibacterial activity are oil-soluble organosulfur compounds that include allicin, ajoenes, and allyl sulfides. The organosulfur compounds of garlic exhibit a range of antibacterial properties such as bactericidal, antibiofilm, antitoxin, and anti-quorum sensing activity against a wide range of bacteria including multi-drug resistant (MDR) strains. The reactive organosulfur compounds form disulfide bonds with free sulfhydryl groups of enzymes and compromise the integrity of the bacterial membrane. The World Health Organization (WHO) has recognized the development of antibiotic resistance as a global health concern and emphasizes antibiotic stewardship along with the urgent need to develop novel antibiotics. Multiple antibacterial effects of organosulfur compounds provide an excellent framework to develop them into novel antibiotics. The review provides a focused and comprehensive portrait of the status of garlic and its compounds as antibacterial agents. In addition, the emerging role of new technologies to harness the potential of garlic as a novel antibacterial agent is discussed.

scholarly journals Antibacterial Activities of Selected Cameroonian Plants and Their Synergistic Effects with Antibiotics against Bacteria Expressing MDR Phenotypes

2012 ◽  
Vol 2012 ◽  
pp. 1-11 ◽  
Author(s):  
Stephen T. Lacmata ◽  
Victor Kuete ◽  
Jean P. Dzoyem ◽  
Simplice B. Tankeo ◽  
Gerald Ngo Teke ◽  
...  
Keyword(s):  
Medicinal Plants ◽  
Bacterial Infections ◽  
Synergistic Effects ◽  
Antibacterial Properties ◽  
Efflux Pumps ◽  
Antibacterial Activities ◽  
Garcinia Kola ◽  
Active Efflux ◽  
Minimal Inhibitory Concentrations ◽  
Methanol Extracts

The present work was designed to assess the antibacterial properties of the methanol extracts of some Cameroonian medicinal plants and the effect of their associations with currently used antibiotics on multidrug resistant (MDR) Gram-negative bacteria overexpressing active efflux pumps. The antibacterial activities of twelve methanol extracts of medicinal plants were evaluated using broth microdilution. The results of this test showed that three extractsGarcinia lucidawith the minimal inhibitory concentrations (MIC) varying from 128 to 512 μg/mL,Garcinia kola(MIC of 256 to 1024 μg/mL), andPicralima nitida(MIC of 128 to 1024 μg/mL) were active on all the twenty-nine studied bacteria including MDR phenotypes. The association of phenylalanine arginineβ-naphthylamide (PAβN or efflux pumps inhibitor) to different extracts did not modify their activities. At the concentration of MIC/2 and MIC/5, the extracts ofP. nitidaandG. kolaimproved the antibacterial activities of some commonly used antibiotics suggesting their synergistic effects with the tested antibiotics. The results of this study suggest that the tested plant extracts and mostly those fromP. nitida,G. lucidaandG. kolacould be used alone or in association with common antibiotics in the fight of bacterial infections involving MDR strains.

Design and Discovery of New Antibacterial Agents: Advances, Perspectives, Challenges

2019 ◽  
Vol 25 (38) ◽  
pp. 4972-5006 ◽  
Author(s):  
Josef Jampilek
Keyword(s):  
Small Molecules ◽  
Bacterial Infections ◽  
Antibacterial Agents ◽  
Bacterial Resistance ◽  
Antibacterial Properties ◽  
Molecular Scaffolds ◽  
Antibacterial Compounds ◽  
Drug Classes ◽  
First Choice ◽  
Wide Range

Background: Emerging resistance of bacterial pathogens to clinically used drugs, including not only first-choice but also second- and third-choice drugs, is alarming, but since the 1990s only a modest number of new, first in class, drugs for systemic administration have been marketed for the treatment of bacterial infections. Objective: This article provides a review of recently reported new antibacterial chemotherapeutics approved for clinical practice, antibacterial chemotherapeutics in clinical trials and antibacterial agents under development. Discussion: Antibacterial agents include new antibacterial compounds of used drug classes and new antibacterial agents with a novel mode of action. In addition, particular attention is given to agents decreasing bacterial resistance, i.e. to compounds that do not have significant intrinsic bacteriostatic or bactericidal activity, but in combination with antibacterial drugs are able to restore the effect of these drugs or demonstrate synergistic antibacterial properties together with the drugs. Conclusion: This review is specifically focused on small molecules rather than on peptides and discusses a wide range of various molecular scaffolds.

scholarly journals Repurposing Avermectins and Milbemycins against Mycobacteroides abscessus and Other Nontuberculous Mycobacteria

Antibiotics ◽  
2021 ◽  
Vol 10 (4) ◽  
pp. 381
Author(s):  
Lara Muñoz-Muñoz ◽  
Carolyn Shoen ◽  
Gaye Sweet ◽  
Asunción Vitoria ◽  
Tim J. Bull ◽  
...  
Keyword(s):  
Nontuberculous Mycobacteria ◽  
Mycobacterium Ulcerans ◽  
Health Concern ◽  
Macrocyclic Lactones ◽  
Wide Range ◽  
Poor Treatment ◽  
Spectrum Activity ◽  
Time Kill ◽  
Broad Spectrum Activity

Infections caused by nontuberculous mycobacteria (NTM) are increasing worldwide, resulting in a new global health concern. NTM treatment is complex and requires combinations of several drugs for lengthy periods. In spite of this, NTM disease is often associated with poor treatment outcomes. The anti-parasitic family of macrocyclic lactones (ML) (divided in two subfamilies: avermectins and milbemycins) was previously described as having activity against mycobacteria, including Mycobacterium tuberculosis, Mycobacterium ulcerans, and Mycobacterium marinum, among others. Here, we aimed to characterize the in vitro anti-mycobacterial activity of ML against a wide range of NTM species, including Mycobacteroides abscessus. For this, Minimum Inhibitory Concentration (MIC) values of eight ML were determined against 80 strains belonging to nine different NTM species. Macrocyclic lactones showed variable ranges of anti-mycobacterial activity that were compound and species-dependent. Milbemycin oxime was the most active compound, displaying broad-spectrum activity with MIC lower than 8 mg/L. Time kill assays confirmed MIC data and showed bactericidal and sterilizing activity of some compounds. Macrocyclic lactones are available in many formulations and have been extensively used in veterinary and human medicine with suitable pharmacokinetics and safety properties. This information could be exploited to explore repurposing of anti-helminthics for NTM therapy.

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