Design, synthesis, characterization, antimicrobial evaluations and molecular docking studies of 5-(phenylcarbamoyl)pentylselenyl tethered ester, acid and trans -β-lactams DOI
Dipika Narula,

Shamsher S. Bari,

Love Singla

et al.

Journal of Sulfur Chemistry, Journal Year: 2024, Volume and Issue: unknown, P. 1 - 20

Published: Dec. 10, 2024

Herein, we unveil the utility of bis(5-phenylcarbamoylpentyl)diselenide 2 for obtaining unique seleno-ester viz ethyl 2-(5-(phenylcarbamoyl)pentylselenyl)ethanoate 3 and further transformation to 2-(5-(phenylcarbamoyl)pentylselenyl)ethanoic acid 4. Next, time-efficient (complete in 15 min.) stereoselective synthesis trans-3-((5-phenylcarbamoyl)pentylselenyl)-β-lactams 6a-d (52-78% yields) starting from seleno-acid 4 substituted imines 5a-d has been reported with relevant characterization data (FT-IR, FT-NMR (1H, 13C), CHN elemental analysis). In vitro antibacterial antifungal biological evaluation silico molecular docking studies exhibit a profound dependence on nature functionality (functionalized selenyl- /ester / β-lactam) anchored 5-(phenylcarbamoyl)pentylselenyl chain. antimicrobial evidenced trans-seleno-β-lactam 6c (incorporating p-methoxyphenyl substituents both at N1 C4 atoms β-lactam ring) be active against all tested gram positive bacterial (S. aureus, B. subtilis), negative (E. coli, P. aeruginosa) fungal (C. albicans) species exhibiting 9-20 mm 8-12 diameter inhibition zones. trans-β-Lactam 6b (with C4-phenyl N1-p-methylphenyl groups) exhibited maximum zone (14 S. aureus) amongst trans-6a-d. Molecular results ligand binding affinity are observed well agreement making these seleno-compounds potential candidates medicinal importance.

Language: Английский

Mycobacterium abscessus: It’s Complex DOI Creative Commons
Hazem F. M. Abdelaal, Edward D. Chan, Lisa Young

et al.

Microorganisms, Journal Year: 2022, Volume and Issue: 10(7), P. 1454 - 1454

Published: July 19, 2022

(

Citations

40
Ampicillin-resistant bacterial pathogens targeted chitosan nano-drug delivery system (CS-AMP-P-ZnO) for combinational antibacterial treatment DOI
Anbazhagan Sathiyaseelan, Kandasamy Saravanakumar, Xin Zhang

et al.

International Journal of Biological Macromolecules, Journal Year: 2023, Volume and Issue: 237, P. 124129 - 124129

Published: March 21, 2023

Language: Английский

Citations

36
Complexes of β-lactam antibiotics and their Schiff-base derivatives as a weapon in the fight against bacterial resistance DOI
Michał Zabiszak, Justyna Frymark, Kazuma Ogawa

et al.

Coordination Chemistry Reviews, Journal Year: 2023, Volume and Issue: 493, P. 215326 - 215326

Published: July 4, 2023

Language: Английский

Citations

29
Navigating Antibacterial Frontiers: A Panoramic Exploration of Antibacterial Landscapes, Resistance Mechanisms, and Emerging Therapeutic Strategies DOI Creative Commons

Krittika Ralhan,

Kavita A. Iyer, Leilani Lotti Díaz

et al.

ACS Infectious Diseases, Journal Year: 2024, Volume and Issue: 10(5), P. 1483 - 1519

Published: May 1, 2024

The development of effective antibacterial solutions has become paramount in maintaining global health this era increasing bacterial threats and rampant antibiotic resistance. Traditional antibiotics have played a significant role combating infections throughout history. However, the emergence novel resistant strains necessitates constant innovation research. We analyzed data on antibacterials from CAS Content Collection, largest human-curated collection published scientific knowledge, which proven valuable for quantitative analysis knowledge. Our focuses mining Collection recent publications (since 2012). This article aims to explore intricate landscape research while reviewing advancement traditional emerging strategies. By delving into resistance mechanisms, paper highlights need find alternate strategies address growing concern.

Language: Английский

Citations

16
Antibiotics: From Mechanism of Action to Resistance and Beyond DOI
Shyamalima Saikia, Pankaj Chetia

Indian Journal of Microbiology, Journal Year: 2024, Volume and Issue: 64(3), P. 821 - 845

Published: April 29, 2024

Language: Английский

Citations

11
Chitosan/Alginate-Based Nanoparticles for Antibacterial Agents Delivery DOI Creative Commons
Nasrul Wathoni, Yedi Herdiana, Cecep Suhandi

et al.

International Journal of Nanomedicine, Journal Year: 2024, Volume and Issue: Volume 19, P. 5021 - 5044

Published: May 1, 2024

Nanoparticle systems integrating alginate and chitosan emerge as a promising avenue to tackle challenges in leveraging the potency of pharmacological active agents. Owing their intrinsic properties polysaccharides, chitosan, exhibit remarkable biocompatibility, rendering them conducive bodily integration. By downsizing drug particles nano-scale, system enhances solubility aqueous environments by augmenting surface area. Additionally, orchestrates extended release kinetics, aligning well with exigencies chronic requisite for antibacterial therapeutics. A thorough scrutiny existing literature underscores wealth evidence supporting utilization alginate-chitosan nanoparticle agent delivery. Literature reviews present abundant based on combination Various experiments demonstrate enhanced efficacy, including an increase inhibitory zone diameter, improvement minimum concentration, enhancement bacterial reduction rate. This efficacy occurs due mechanisms involving increased resulting from particle size reduction, prolonged effects, selectivity towards cell walls, stemming ionic interactions between positively charged teichoic acid walls. However, clinical studies remain limited, there are currently no marketed drugs utilizing this system. Hence, expediting validation is crucial maximize its benefits promptly.

Language: Английский

Citations

11
Target Identification in Anti-Tuberculosis Drug Discovery DOI Open Access
Rita Capela, Rita Félix, Marta Clariano

et al.

International Journal of Molecular Sciences, Journal Year: 2023, Volume and Issue: 24(13), P. 10482 - 10482

Published: June 22, 2023

Mycobacterium tuberculosis (Mtb) is the etiological agent of (TB), a disease that, although preventable and curable, remains global epidemic due to emergence resistance latent form responsible for long period treatment. Drug discovery in TB challenging task heterogeneity disease, resistance, uncomplete knowledge pathophysiology disease. The limited permeability cell wall presence multiple efflux pumps remain major barrier achieve effective intracellular drug accumulation. While complete genome sequence Mtb has been determined several potential protein targets have validated, lack adequate models vitro vivo studies limiting factor programs. In current therapeutic regimens, less than 0.5% bacterial proteins are targeted during biosynthesis energetic metabolism two most important processes exploited chemotherapeutics. This review provides an overview on challenges emerging druggable proteins, explains how chemical probes profiling enabled identification new biomarkers, paving way disruptive regimens diagnostic tools.

Language: Английский

Citations

19
Novel synergistic interactions between monolaurin, a mono-acyl glycerol and β lactam antibiotics against Staphylococcus aureus: an in vitro study DOI Creative Commons

Shimaa Salah Hassan Abd El Ghany,

Reham Ali Ibrahem,

Ahmed O. El‐Gendy

et al.

BMC Infectious Diseases, Journal Year: 2024, Volume and Issue: 24(1)

Published: April 8, 2024

Abstract Background A major worldwide health issue is the rising frequency of resistance bacteria.Drug combinations are a winning strategy in fighting resistant bacteria and might help protecting existing drugs.Monolaurin natural compound extracted from coconut oil has promising antimicrobial activity against Staphylococcus.aureus . This study aims to examine efficacy monolaurin both individually combination with β-lactam antibiotics Staphylococcus aureus isolates. Methods Agar dilution method was used for determination minimum inhibitory concentration (MIC) S.aureus Scanning electron microscope (SEM) detect morphological changes after treatment monolaurin. Conventional Real-time Polymerase chain reaction (RT-PCR) were performed beta-lactamase (blaZ) gene its expressional levels treatment. Combination therapy assessed through fractional time-kill method. Results The antibacterial on 115 isolates, MIC 250 2000 µg/ml. SEM showed cell elongation swelling outer membrane prescence 1xMIC bla Z found 73.9% RT-PCR shows significant decrease blaZ expression at 500 µg/ml Synergistic effects detected FIC time killing curve. established reduction value. collective findings antibiotic indicated synergism rates ranging 83.3% 100%.In studies, produced synergistic effect. Conclusion that may be agent S. , an outstanding modulator drugs. concurrent application antibiotics, exhibiting vitro, holds promise as potential candidates development therapies target particularly, patients bacterial infections nearly incurable.

Language: Английский

Citations

7
Novel Penicillin Derivatives Against Selected Multiple-drug Resistant Bacterial Strains: Design, Synthesis, Structural Analysis, In Silico and In Vitro Studies DOI
Aso Hameed Hasan, Narmin Hamaamin Hussen, Shokhan Jamal Hamid

et al.

Current Organic Synthesis, Journal Year: 2023, Volume and Issue: 21(5), P. 684 - 703

Published: May 11, 2023

The rising numbers of multiple drug-resistant (MDR) pathogens and the consequent antibacterial therapy failure that resulted in severe medical conditions push to illustrate new molecules with extended activity against resistant strains. In this manner, chemical derivatization known antibiotics is proposed save efforts drug discovery, penicillins serve as an ideal regard.

Language: Английский

Citations

11
Insights into the Microbiome and Antibiotic Resistance Genes from Hospital Environmental Surfaces: A Prime Source of Antimicrobial Resistance DOI Creative Commons
Alfizah Hanafiah, Asif Sukri,

Hamidah Yusoff

et al.

Antibiotics, Journal Year: 2024, Volume and Issue: 13(2), P. 127 - 127

Published: Jan. 26, 2024

Hospital environmental surfaces are potential reservoirs for transmitting hospital-associated pathogens. This study aimed to profile microbiomes and antibiotic resistance genes (ARGs) from hospital using 16S rRNA amplicon metagenomic sequencing at a tertiary teaching in Malaysia. Samples were collected patient sinks healthcare staff counters surgery orthopaedic wards. The samples’ DNA subjected shotgun identify bacterial taxonomic profiles, genes, virulence factor pathways. richness was more diverse the samples than those counters. Proteobacteria Verrucomicrobia dominated phylum level, while Bacillus, Staphylococcus, Pseudomonas, Acinetobacter genus level. Staphylococcus epidermidis aureus prevalent on Bacillus cereus counter samples. highest counts of ARGs beta-lactam detected, followed by against fosfomycin cephalosporin. We report detection mcr-10.1 that confers colistin setting gene pathways aid transfer between bacteria identified. Environmental serve as nosocomial infections require mitigation strategies control spread bacteria.

Language: Английский

Citations

4