Biological investigation of N-methyl thiosemicarbazones as antimicrobial agents and bacterial carbonic anhydrases inhibitors

Journal of Enzyme Inhibition and Medicinal Chemistry, Journal Year: 2022, Volume and Issue: 37(1), P. 986 - 993

Published: March 24, 2022

The enormous burden of the COVID-19 pandemic in economic and healthcare terms has cast a shadow on serious threat antimicrobial resistance, increasing inappropriate use antibiotics shifting focus drug discovery programmes from antibacterial antifungal fields. Thus, there is pressing need for new antimicrobials involving innovative modes action (MoAs) to avoid cross-resistance rise. Thiosemicarbazones (TSCs) stand out due their easy preparation polypharmacological application, also infectious diseases. Recently, we reported small library TSCs (1-9) that emerged non-cytotoxic behaviour. Inspired by multifaceted activity, investigated antibacterial, antifungal, antidermatophytal profiles derivatives 1-9, highlighting promising research line. Furthermore, ability these compounds inhibit selected microbial human carbonic anhydrases (CAs) was assessed, revealing possible involvement MoA good selectivity index some derivatives.

Language: Английский

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Microplastics and other emerging contaminants in the environment after COVID-19 pandemic: The need of global reconnaissance studies

Current Opinion in Environmental Science & Health, Journal Year: 2023, Volume and Issue: 33, P. 100468 - 100468

Published: April 11, 2023

Language: Английский

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Antibiofilm and Anti-Quorum-Sensing Activities of Novel Pyrazole and Pyrazolo[1,5-a]pyrimidine Derivatives as Carbonic Anhydrase I and II Inhibitors: Design, Synthesis, Radiosterilization, and Molecular Docking Studies

Antibiotics, Journal Year: 2023, Volume and Issue: 12(1), P. 128 - 128

Published: Jan. 9, 2023

Nowadays, searching for new anti-infective agents with diverse mechanisms of action has become necessary. In this study, 16 pyrazole and pyrazolo[1,5-a]pyrimidine derivatives were synthesized assessed their preliminary antibacterial antibiofilm activities. All these initially screened activity against six clinically isolated multidrug resistance by agar well-diffusion broth microdilution methods. The initial screening presented significant a bactericidal effect five compounds, namely 3a, 5a, 6, 9a, 10a, compared Erythromycin Amikacin. These further evaluated both S. aureus P. aeruginosa, which showed strong biofilm-forming at MICs >60%. SEM analysis confirmed the biofilm disruption in presence derivatives. Furthermore, anti-QS was observed hybrids sub-MICs, as indicated visible halo zone. addition, most active reduces violacein production CV026, confirming that compounds yielded activity. inhibitory human carbonic anhydrase (hCA-I hCA-II) isoforms IC50 values ranging between 92.34 168.84 nM 73.2 161.22 nM, respectively. Finally, radiosterilization, ADMET, docking simulation performed.

Language: Английский

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Prevalence of pharmaceuticals and personal care products, microplastics and co-infecting microbes in the post-COVID-19 era and its implications on antimicrobial resistance and potential endocrine disruptive effects

The Science of The Total Environment, Journal Year: 2023, Volume and Issue: 904, P. 166419 - 166419

Published: Aug. 23, 2023

Language: Английский

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Antibiotic-Resistant ESKAPE Pathogens and COVID-19: The Pandemic beyond the Pandemic

Viruses, Journal Year: 2023, Volume and Issue: 15(9), P. 1843 - 1843

Published: Aug. 30, 2023

Antibacterial resistance is a renewed public health plague in modern times, and the COVID-19 pandemic has rekindled this problem. Changes antibiotic prescribing behavior, misinformation, financial hardship, environmental impact, governance gaps have generally enhanced misuse improper access to antibiotics during pandemic. These determinants, intersected with antibacterial current pandemic, may amplify potential for future The occurrence of infections multidrug-resistant (MDR), extensively drug-resistant (XDR), difficult-to-treat (DTR), carbapenem-resistant (CR), pan-drug-resistant (PDR) bacteria still increasing. aim review highlight state art worldwide, focusing on most important pathogens, namely Enterobacterales, Acinetobacter baumannii, Klebsiella pneumoniae, their common antibiotics.

Language: Английский

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Antimicrobial resistance burden pre and post-COVID-19 pandemic with mapping the multidrug resistance in Egypt: a comparative cross-sectional study

Scientific Reports, Journal Year: 2024, Volume and Issue: 14(1)

Published: March 26, 2024

Abstract Overuse of antibiotics during coronavirus disease 2019 (COVID-19) in an attempt to reduce COVID-19 mortality the short term may have contributed long-term from antimicrobial resistance (AMR). The aim this study was evaluate impact pandemic on AMR Egypt and map distribution multidrug-resistant (MDR) extensive drug-resistant (XDR) across Egypt. Through a multicenter cross-sectional 2430 culture results were collected 2022 pre post-COVID-19 Egypt, including 400 Klebsiella pneumoniae, 760 Escherichia coli , 650 Acinetobacter baumannii 620 Methicillin-resistant staphylococcus aureus (MRSA) results. MDR XDR highlighted through geographic information system. Mixed effect logistic regression models sub-group analysis performed according type specimens test resistance. Adjusted demonstrated K. pneumoniae has increased against quinolones carbapenems ( P < 0.001). Resistance E. significantly imipenem meropenem. While E.coli susceptibility cefoxitin, levofloxacin, ciprofloxacin. A. more than double ceftazidime, cefepime, piperacillin-tazobactam MRSA reserved its vancomycin linezolid. 67% 94% 79% 98%, respectively 6% 46%, 47% 69%, changed profile so that urgent action is required mitigate threat preserve our capacity face infections future decades.

Language: Английский

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Antimicrobial resistance (AMR) management using CRISPR-Cas based genome editing

Gene and Genome Editing, Journal Year: 2024, Volume and Issue: 7, P. 100031 - 100031

Published: Jan. 9, 2024

Antimicrobial resistance is a serious threat to the human population and might be responsible for emergence as well re-emergence of various infectious diseases. The staggard development new antibiotics acquired by pathogens against existing indeed menace has aggravated due present pandemic. CRISPR-Cas systems, an inherent immune mechanism in prokaryotes one most popular tools that was first harnessed 2014 selective removal genes antimicrobial resistance. Gradually gaining considerable momentum field genetics, medicine, biotechnology, technologies have been rapidly utilized gene editing cells, designing animal models disease progression studies develop insect-resistant crop varieties repurpose bacterial systems target specific elimination pathogens. main aim this review discuss how produce new-generation antimicrobials, associated delivery vehicles challenges, prospects these powerful antimicrobials.

Language: Английский

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TiO2 nanotube arrays photocatalytic ozonation for the removal of antibiotic ciprofloxacin from the effluent of a domestic wastewater treatment plant: Towards the process upscaling

Journal of Water Process Engineering, Journal Year: 2024, Volume and Issue: 63, P. 105457 - 105457

Published: May 21, 2024

Language: Английский

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Synthetic Star Nanoengineered Antimicrobial Polymers as Antibiofilm Agents: Bacterial Membrane Disruption and Cell Aggregation

Biomacromolecules, Journal Year: 2023, Volume and Issue: 24(7), P. 3073 - 3085

Published: June 10, 2023

Antimicrobial resistance has become a worldwide issue, with multiresistant bacterial strains emerging at an alarming rate. Multivalent antimicrobial polymer architectures such as bottle brush or star polymers have shown great potential, they could lead to enhanced binding and interaction the cell membrane. In this study, library of amphiphilic copolymers their linear copolymer equivalents, based on acrylamide monomers, were synthesized via RAFT polymerization. Their monomer distribution molecular weight varied. Subsequently, activity toward Gram-negative bacterium (Pseudomonas aeruginosa PA14) Gram-positive (Staphylococcus aureus USA300) hemocompatibility investigated. The statistical copolymer, S-SP25, showed improved compared its equivalent againstP. aeruginosaPA14. architecture activity, causing aggregation, revealed electron microscopy. However, it also induced increased red blood aggregation equivalents. Changing/shifting position cationic block core structure prevents effect while maintaining potent for smallest copolymer. Finally, compound antibiofilm properties against robust in vitro biofilm model.

Language: Английский

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A 7-Year Brazilian National Perspective on Plasmid-Mediated Carbapenem Resistance in Enterobacterales, Pseudomonas aeruginosa, and Acinetobacter baumannii Complex and the Impact of the Coronavirus Disease 2019 Pandemic on Their Occurrence

Clinical Infectious Diseases, Journal Year: 2023, Volume and Issue: 77(Supplement_1), P. S29 - S37

Published: July 1, 2023

Abstract Background Carbapenemase production is a global public health threat. Antimicrobial resistance (AMR) data analysis critical to policy. Here we analyzed carbapenemase detection trends using the AMR Brazilian Surveillance Network. Methods from hospitals included in laboratory information system dataset were evaluated. The rate (DR) was defined as detected by gene tested per isolate year. temporal estimated Prais–Winsten regression model. impact of COVID-19 on genes Brazil determined for period 2015–2022. Detection pre- (October 2017 March 2020) and post-pandemic onset (April 2020 September 2022) compared χ2 test. Analyses performed with Stata 17.0 (StataCorp, College Station, TX). Results 83 282 blaKPC 86 038 blaNDM all microorganisms. Enterobacterales DR 68.6% (41 301/60 205) 14.4% (8377/58 172), respectively. P. aeruginosa 2.5% (313/12 528). An annual percent increase 41.1% observed, decrease −4.0% Enterobacterales, an 71.6% 22.2% aeruginosa. From 2022, overall increases 65.2% 77.7% ABC, 61.3% observed total isolates. Conclusions This study shows strengths Network robust related carbapenemases change profiles rising over years.

Language: Английский

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