scholarly journals Antimicrobial activity of some novel 2-(2-iodophenylimino)-5-arylidenethiazolidin-4-one derivatives

2018 ◽  
Vol 11 (5) ◽  
pp. 405-412 ◽  
Author(s):  
Duy Toan Pham ◽  
Thi My Huong Vo ◽  
Phuong Truong ◽  
Phuoc Tinh Ho ◽  
Manh Quan Nguyen
Keyword(s):  
Antimicrobial Activity ◽  
Aldol Condensation ◽  
Antibacterial Activities ◽  
Multidrug Resistant ◽  
Therapeutic Agents ◽  
Antifungal Drugs ◽  
Resistant Bacteria ◽  
Bacterial Strains ◽  
Synthetic Process ◽  
New Compounds

AbstractBackgroundInfectious diseases, especially those caused by multidrug-resistant bacteria, are becoming a serious problem worldwide because of the lack of effective therapeutic agents. Moreover, most antifungal drugs exhibit low efficacy and high toxicity because of the similarity between fungal and human cells. These issues warrant the search for potential new agents.ObjectivesTo synthesize potent 2-(2-iodophenylimino)-5-arylidenethiazolidin-4-one derivatives, improve the synthetic process, elucidate their structures, and determine their antimicrobial activity.Methods2-Iodoaniline was used as an initial reactant in a 3-step process for the synthesis of 2-(2-iodophenylimino)-5-arylidenethiazolidin-4-one derivatives, including an acylation reaction, a cyclization reaction, and aldol condensation reactions. The structures of the obtained derivatives were investigated and elucidated using spectral methods. Antimicrobial activity toward 5 bacterial strains and 2 fungal strains was determined using Kirby–Bauer and agar dilution methods.ResultsWe successfully synthesized 12 novel compounds and elucidated their structures. The derivatives had no antifungal activities. By contrast, they showed remarkable antibacterial activities. Some of them with minimum inhibitory concentrations (MICs) ≤8 μg/mL in both Staphylococcus aureus and methicillin-resistant S. aureus.ConclusionsA simple and flexible way to synthesize new compounds with a thiazolidin-4-one ring was determined. Some of these new compounds have outstanding effects with low MICs for bacteria. Their further investigation as therapeutic agents is warranted.

scholarly journals Transcriptome Analysis of Psacothea hilaris: De Novo Assembly and Antimicrobial Peptide Prediction

Insects ◽  
2020 ◽  
Vol 11 (10) ◽  
pp. 676 ◽  
Author(s):  
Joon Ha Lee ◽  
Hoyong Chung ◽  
Yong Pyo Shin ◽  
In-Woo Kim ◽  
Sathishkumar Natarajan ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Peptide ◽  
De Novo ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Bacterial Strains ◽  
Illumina Platform ◽  
E Coli ◽  
Innate Defense

Antimicrobial peptides (AMPs) are the frontline innate defense system evolutionarily preserved in insects to combat invading pathogens. These AMPs could serve as an alternative to classical antibiotics to overcome the burden of treating multidrug resistant bacteria. Psacotheasin, a knottin type AMP was isolated from Psacothea hilaris and shown to exhibit antimicrobial activity, especially against fungi through apoptosis mediated cell death. In this study, we aimed to identify novel probable AMPs from Psacothea hilaris, the yellow spotted longicorn beetle. The beetle was immunized with the two bacterial strains (E. coli and S. aureus), and the yeast strain C. albicans. After immunization, total RNA was isolated and sequenced in Illumina platform. Then, beetle transcriptome was de novo assembled and searched for putative AMPs with the known physiochemical features of the AMPs. A selection of AMP candidates were synthesized and tested for antimicrobial activity. Four peptides showed stronger activity against E. coli than the control AMP, melittin while one peptide showed similar activity against S. aureus. Moreover, four peptides and two peptides showed antifungal activity stronger than and similar to melittin, respectively. Collectively one peptide showed both antibacterial and antifungal activity superior to melittin; thus, it provides a potent antimicrobial peptide. All the peptides showed no hemolysis in all the tested concentrations. These results suggest that in silico mining of insects’ transcriptome could be a promising tool to obtain and optimize novel AMPs for human needs.

scholarly journals Multistep optimization of a cell-penetrating peptide towards its antimicrobial activity

2020 ◽  
Author(s):  
Marco Drexelius ◽  
André Reinhardt ◽  
Joshua Grabeck ◽  
Tom Cronenberg ◽  
Frank Nitsche ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Mammalian Cells ◽  
Building Blocks ◽  
Physicochemical Characteristics ◽  
Antibacterial Activities ◽  
Multidrug Resistant ◽  
Cell Penetrating Peptides ◽  
Bacterial Strains ◽  
Cell Penetrating ◽  
Promising Source

Multidrug resistant (MDR) bacteria have adapted to most clinical antibiotics and are a growing threat to human health. One promising type of candidates for the everlasting demand of new antibiotic compounds constitute antimicrobial peptides (AMPs). These peptides act against different types of microbes by permeabilizing pathogen cell membranes, whereas being harmless to mammalian cells. Contrarily, another class of membrane-active peptides, namely cell-penetrating peptides (CPPs), is known to translocate in eukaryotic cells without substantially affecting the cell membrane. Since CPPs and AMPs share several physicochemical characteristics, we hypothesized if we can rationally direct the activity of a CPP towards antimicrobial activity. Herein, we describe the screening of a synthetic library, based on the CPP sC18, including structure-based design to identify the active residues within a CPP sequence and to discover novel AMPs with high activity. Peptides with increased hydrophobicity were tested against various bacterial strains, and hits were further optimized leading to four generations of peptides, with the last also comprising fluorinated amino acid building blocks. Interestingly, beside strong antibacterial activities, we also detected activity in cancer cells, while non-cancerous cells remained unharmed. The results highlight our new candidates, particularly those from generation 4, as a valuable and promising source for the development of future therapeutics with antibacterial activity and beyond.

scholarly journals Rhamnolipids Nano-Micelles as a Potential Hand Sanitizer

Antibiotics ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 751
Author(s):  
Marwa Reda Bakkar ◽  
Ahmed Hassan Ibrahim Faraag ◽  
Elham R. S. Soliman ◽  
Manar S. Fouda ◽  
Amir Mahfouz Mokhtar Sarguos ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Active Sites ◽  
Specific Interaction ◽  
Virus Transmission ◽  
Multidrug Resistant ◽  
Future Perspective ◽  
Resistant Bacteria ◽  
In Silico Studies

COVID-19 is a pandemic disease caused by the SARS-CoV-2, which continues to cause global health and economic problems since emerging in China in late 2019. Until now, there are no standard antiviral treatments. Thus, several strategies were adopted to minimize virus transmission, such as social distancing, face covering protection and hand hygiene. Rhamnolipids are glycolipids produced formally by Pseudomonas aeruginosa and as biosurfactants, they were shown to have broad antimicrobial activity. In this study, we investigated the antimicrobial activity of rhamnolipids against selected multidrug resistant bacteria and SARS-CoV-2. Rhamnolipids were produced by growing Pseudomonas aeruginosa strain LeS3 in a new medium formulated from chicken carcass soup. The isolated rhamnolipids were characterized for their molecular composition, formulated into nano-micelles, and the antibacterial activity of the nano-micelles was demonstrated in vitro against both Gram-negative and Gram-positive drug resistant bacteria. In silico studies docking rhamnolipids to structural and non-structural proteins of SARS-CoV-2 was also performed. We demonstrated the efficient and specific interaction of rhamnolipids with the active sites of these proteins. Additionally, the computational studies suggested that rhamnolipids have membrane permeability activity. Thus, the obtained results indicate that SARS-CoV-2 could be another target of rhamnolipids and could find utility in the fight against COVID-19, a future perspective to be considered.

scholarly journals Sulfaguanidine Hybrid with Some New Pyridine-2-One Derivatives: Design, Synthesis, and Antimicrobial Activity against Multidrug-Resistant Bacteria as Dual DNA Gyrase and DHFR Inhibitors

Antibiotics ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 162
Author(s):  
Ahmed Ragab ◽  
Sawsan A. Fouad ◽  
Ola A. Abu Ali ◽  
Entsar M. Ahmed ◽  
Abeer M. Ali ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Fungal Growth ◽  
Dna Gyrase ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Design Synthesis ◽  
Potent Inhibition ◽  
Ic50 Values ◽  
Dhfr Inhibitors ◽  
Positive Controls

Herein, a series of novel hybrid sulfaguanidine moieties, bearing 2-cyanoacrylamide 2a–d, pyridine-2-one 3–10, and 2-imino-2H-chromene-3-carboxamide 11, 12 derivatives, were synthesized, and their structure confirmed by spectral data and elemental analysis. All the synthesized compounds showed moderate to good antimicrobial activity against eight pathogens. The most promising six derivatives, 2a, 2b, 2d, 3a, 8, and 11, revealed to be best in inhibiting bacterial and fungal growth, thus showing bactericidal and fungicidal activity. These derivatives exhibited moderate to potent inhibition against DNA gyrase and DHFR enzymes, with three derivatives 2d, 3a, and 2a demonstrating inhibition of DNA gyrase, with IC50 values of 18.17–23.87 µM, and of DHFR, with IC50 values of 4.33–5.54 µM; their potency is near to that of the positive controls. Further, the six derivatives exhibited immunomodulatory potential and three derivatives, 2d, 8, and 11, were selected for further study and displayed an increase in spleen and thymus weight and enhanced the activation of CD4+ and CD8+ T lymphocytes. Finally, molecular docking and some AMED studies were performed.

scholarly journals Antimicrobial Activity of Cyclic-Monomeric and Dimeric Derivatives of the Snail-Derived Peptide Cm-p5 against Viral and Multidrug-Resistant Bacterial Strains

Biomolecules ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 745
Author(s):  
Melaine González-García ◽  
Fidel Morales-Vicente ◽  
Erbio Díaz Pico ◽  
Hilda Garay ◽  
Daniel G. Rivera ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Multidrug Resistant ◽  
Moderate Activity ◽  
Dependent Manner ◽  
Bacterial Strains ◽  
Acinetobacter Baumanii ◽  
Concentration Dependent Manner ◽  
Conventional Antibiotics

Cm-p5 is a snail-derived antimicrobial peptide, which demonstrated antifungal activity against the pathogenic strains of Candida albicans. Previously we synthetized a cyclic monomer as well as a parallel and an antiparallel dimer of Cm-p5 with improved antifungal activity. Considering the alarming increase of microbial resistance to conventional antibiotics, here we evaluated the antimicrobial activity of these derivatives against multiresistant and problematic bacteria and against important viral agents. The three peptides showed a moderate activity against Pseudomonas aeruginosa, Klebsiella pneumoniae Extended Spectrum β-Lactamase (ESBL), and Streptococcus agalactiae, with MIC values > 100 µg/mL. They exerted a considerable activity with MIC values between 25–50 µg/mL against Acinetobacter baumanii and Enterococcus faecium. In addition, the two dimers showed a moderate activity against Pseudomonas aeruginosa PA14. The three Cm-p5 derivatives inhibited a virulent extracellular strain of Mycobacterium tuberculosis, in a dose-dependent manner. Moreover, they inhibited Herpes Simplex Virus 2 (HSV-2) infection in a concentration-dependent manner, but had no effect on infection by the Zika Virus (ZIKV) or pseudoparticles of Severe Acute Respiratory Syndrome Corona Virus 2 (SARS-CoV-2). At concentrations of >100 µg/mL, the three new Cm-p5 derivatives showed toxicity on different eukaryotic cells tested. Considering a certain cell toxicity but a potential interesting activity against the multiresistant strains of bacteria and HSV-2, our compounds require future structural optimization.

scholarly journals Synthesis, Structure Elucidation, Antibacterial Activities, and Synergistic Effects of Novel Juglone and Naphthazarin Derivatives Against Clinical Methicillin-Resistant Staphylococcus aureus Strains

2021 ◽  
Vol 9 ◽  
Author(s):  
Valentin Duvauchelle ◽  
Chaimae Majdi ◽  
David Bénimélis ◽  
Catherine Dunyach-Remy ◽  
Patrick Meffre ◽  
...  
Keyword(s):  
Synergistic Effects ◽  
Antibacterial Properties ◽  
Clinical Importance ◽  
Antibacterial Activities ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Global Public Health ◽  
Gram Positive ◽  
Drug Resistant Bacteria ◽  
Mrsa Strains

Infections caused by drug-resistant bacteria are a serious threat to human and global public health. Moreover, in recent years, very few antibiotics have been discovered and developed by pharmaceutical companies. Therefore, there is an urgent need to discover and develop new antibacterial agents to combat multidrug-resistant bacteria. In this study, two novel series of juglone/naphthazarin derivatives (43 compounds) were synthesized and evaluated for their antibacterial properties against various clinical and reference Gram-positive MSSA, clinical Gram-positive MRSA, and clinical and reference Gram-negative bacteria E. coli and P. aeruginosa. These strains are of clinical importance because they belong to ESKAPE pathogens. Compounds 3al, 5ag, and 3bg showed promising activity against clinical and reference MSSA (MIC: 1–8 µg/ml) and good efficacy against clinical MRSA (MIC: 2–8 µg/ml) strains. 5am and 3bm demonstrated better activity on both MSSA (MIC: 0.5 µg/ml) and MRSA (MIC: 2 µg/ml) strains. Their MICs were similar to those of cloxacillin against clinical MRSA strains. The synergistic effects of active compounds 3al, 5ag, 5am, 3bg, and 3bm were evaluated with reference antibiotics, and it was found that the antibiotic combination with 3bm efficiently enhanced the antimicrobial activity. Compound 3bm was found to restore the sensitivity of clinical MRSA to cloxacillin and enhanced the antibacterial activity of vancomycin when they were added together. In the presence of 3bm, the MIC values of vancomycin and cloxacillin were lowered up to 1/16th of the original MIC with an FIC index of 0.313. Moreover, compounds 3al, 5ag, 5am, 3bg, and 3bm did not present hemolytic activity on sheep red blood cells. In silico prediction of ADME profile parameter results for 3bm is promising and encouraging for further development.

scholarly journals Multidrug Resistant and Extensively Drug Resistant Bacteria: A Study

2016 ◽  
Vol 2016 ◽  
pp. 1-5 ◽  
Author(s):  
Silpi Basak ◽  
Priyanka Singh ◽  
Monali Rajurkar
Keyword(s):  
Antimicrobial Resistance ◽  
Antibiotic Susceptibility ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Close Monitoring ◽  
Care Hospital ◽  
Drug Resistant ◽  
Bacterial Isolates ◽  
Bacterial Strains ◽  
Extensively Drug Resistant

Background and Objective. Antimicrobial resistance is now a major challenge to clinicians for treating patients. Hence, this short term study was undertaken to detect the incidence of multidrug-resistant (MDR), extensively drug-resistant (XDR), and pandrug-resistant (PDR) bacterial isolates in a tertiary care hospital.Material and Methods. The clinical samples were cultured and bacterial strains were identified in the department of microbiology. The antibiotic susceptibility profile of different bacterial isolates was studied to detect MDR, XDR, and PDR bacteria.Results. The antibiotic susceptibility profile of 1060 bacterial strains was studied. 393 (37.1%) bacterial strains were MDR, 146 (13.8%) strains were XDR, and no PDR was isolated. All (100%) Gram negative bacterial strains were sensitive to colistin whereas all (100%) Gram positive bacterial strains were sensitive to vancomycin.Conclusion. Close monitoring of MDR, XDR, or even PDR must be done by all clinical microbiology laboratories to implement effective measures to reduce the menace of antimicrobial resistance.

scholarly journals Chemical Composition, Antioxidant and Antibacterial Activity of Bunium persicum, Eucalyptus globulus, and Rose Water on Multidrug-Resistant Listeria Species

2018 ◽  
Vol 23 ◽  
pp. 2515690X1775131 ◽  
Author(s):  
Farhad Sharafati Chaleshtori ◽  
Mohamad Saholi ◽  
Reza Sharafati Chaleshtori
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Essential Oil ◽  
Essential Oils ◽  
Eucalyptus Globulus ◽  
Multidrug Resistant ◽  
Bacterial Strains ◽  
Antioxidant Power ◽  
Listeria Species ◽  
Bunium Persicum

This research was aimed at investigating the antioxidant and antibacterial activity of Bunium persicum, Eucalyptus globulus, and rose water on multidrug-resistant Listeria species. The antibiotic resistance of Listeria spp obtained from seafood samples were determined by the Kirby-Bauer method. The antioxidant and antibacterial activity of the essential oils and extracts were evaluated using ferric reducing antioxidant power and microdilution methods, respectively. A total 2 samples (1.88%) were positive for Listeria spp. L monocytogenes was found to be resistant to ampicillin, amoxicillin/clavulanic acid, penicillin, vancomycin, and kanamycin. B persicum essential oil showed the greatest antioxidant activity (248.56 ± 1.09 µM Fe2+/g). The E globulus essential oil showed consistently strong antimicrobial activity against L monocytogenes and L grayi, while rose water showed no antimicrobial activity against any of the tested bacterial strains. The results showed that after adding the B persicum and E globulus essential oils to bacteria, the cell components’ release increased significantly.

Comparative Study of Genetic and Antibacterial Profiles of Nigerian Indigenous and Exotic Varieties of Garlic (Allium sativum)

2021 ◽  
Vol 1 (1) ◽  
Author(s):  
Pius A. Okiki ◽  
Oluwafunmilayo Adegbola ◽  
Pius Ade-Ojo ◽  
Amos A. Onasanya ◽  
Olufemi Oyelakin ◽  
...  
Keyword(s):  
Pregnant Women ◽  
Allium Sativum ◽  
Health Benefit ◽  
Antibacterial Activities ◽  
Multidrug Resistant ◽  
Mean Value ◽  
Urine Samples ◽  
Resistant Bacteria ◽  
Methanolic Extracts ◽  
Genetic Profiles

Extracts and isolated compounds of Allium sativum (garlic) have been found to be of health benefit. The study was aimed at assessing the effects of crude garlic extracts on urinopathogens of pregnant women, as well as to compare the antibacterial and genetic profiles of Nigerian indigenous and exotic varieties of garlic. Biodata and urine samples were collected from two hundred (200) healthy pregnant women attending antenatal clinics. The urine samples were subjected to urinalysis and bacteriological investigations. The subjects were 20 - 43 (31.03 ± 1.46) years old, with modal age 25-30 years. Urinalysis of subjects’ urine samples showed no nitrituria, haematuria and bilirubinuria. However, glucosuria (1.5%), ketonuria (3%), leukocyturia (15%) and proteinuria (24%) were detected. Bacterial loads of the urine samples range from 0 to 1100 (with mean value of 315.72) cfU/mL, an indication of non-urinary tract infection bacteriuria. Bacteria isolated from the urine samples were: Escherichia coli, Klebsiella pneumoniae, Klebsiella variicola, Enterobacter cloacae, Pseudomonas aeruginosa, Proteus mirabilis, citrobacter freundii, corynebacterium accolens, Actinomyces urogenitalis, Luteococcus sanguinis and Bacillus cereus among others. The bacterial isolates showed high prevalence of multidrug resistant bacteria, with resistance to 2-8 drugs. The filtrates of crushed and centrifuged bulbs of both the indigenous and exotic varieties of garlic produced high antibacterial activities, while both ethanolic and methanolic extracts of garlic did not produce antibacterial activity. The indigenous variety showed higher antibacterial activities and protein qualities than the exotic variety, with both varieties showing genetic diversity. In conclusion, the Nigerian indigenous garlic was found to be of high antibacterial and protein qualities; and for maximal health benefit garlic needs to be chewed or crushed and consumed directly.

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