Membrane-Targeting Amphiphilic Honokiol Derivatives Containing an Oxazole Moiety as Potential Antibacterials against Methicillin-Resistant Staphylococcus aureus

Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: unknown

Published: Sept. 11, 2024

Infections with methicillin-resistant

Language: Английский

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Plant Flavonoids with Antimicrobial Activity against Methicillin-Resistant Staphylococcus aureus (MRSA)

ACS Infectious Diseases, Journal Year: 2024, Volume and Issue: 10(9), P. 3086 - 3097

Published: June 4, 2024

Methicillin-resistant

Language: Английский

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Unlocking the Antibacterial Potential of Naphthalimide–Coumarins to Overcome Drug Resistance with Antibiofilm and Membrane Disruption Ability against Escherichia coli

ACS Applied Materials & Interfaces, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 7, 2025

Resistance by bacteria to available antibiotics is a threat human health, which demands the development of new antibacterial agents. Considering prevailing conditions, we have developed library naphthalimide-coumarin moieties as broad-spectrum agents fight against awful drug resistance. Preliminary studies indicate that compounds

Language: Английский

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Development of amphipathic derivatives of thymol and carvacrol as potent broad-spectrum antibacterial agents

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 276, P. 116716 - 116716

Published: July 26, 2024

Language: Английский

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Quaternized antimicrobial peptide mimics based on harmane as potent anti-MRSA agents by multi-target mechanism covering cell wall, cell membrane and intracellular targets

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 276, P. 116657 - 116657

Published: July 4, 2024

Language: Английский

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Identification of CH2-linked quinolone-aminopyrimidine hybrids as potent anti-MRSA agents: Low resistance potential and lack of cross-resistance with fluoroquinolone antibiotics

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 271, P. 116399 - 116399

Published: April 11, 2024

Language: Английский

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From Natural Products to Small Molecules: Recent Advancements in Anti-MRSA Therapeutics

ACS Medicinal Chemistry Letters, Journal Year: 2025, Volume and Issue: 16(4), P. 542 - 551

Published: March 14, 2025

The urgent need for unique small molecules to treat increasing resistance in gram-positive pathogens, particularly methicillin-resistant Staphylococcus aureus, has motivated several creative research endeavors over the past decade. Recent advances have been inspired by natural products such as pleuromutilin, discovered high-throughput screens, or repurposed approved drugs like sorafenib. This microperspective spotlights bioactive compounds, ranging from molecule scaffolds, that reported recent literature, highlighting their mechanisms of action, structure-activity relationships, and future potential.

Language: Английский

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Dimeric peptoids as antibacterial agents

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 147, P. 107334 - 107334

Published: April 3, 2024

Building upon our previous study on peptoid-based antibacterials which showed good activity against Gram-positive bacteria only, herein we report the synthesis of 34 dimeric peptoid compounds and investigation their Gram-negative pathogens. The newly designed peptoids feature a di-hydrophobic moiety incorporating phenyl, bromo-phenyl, naphthyl groups, combined with variable lengths cationic units such as amino guanidine groups. also underscores pivotal interplay between hydrophobicity cationicity in optimizing efficacy specific bacteria. bromophenyl guanidinium compound 10j excellent S. aureus 38 E. coli K12 MIC 0.8 μg mL−1 6.2 mL−1, respectively. Further into mechanism action revealed that antibacterial effect might be attributed to disruption bacterial cell membranes, suggested by tethered bilayer lipid membranes (tBLMs) cytoplasmic membrane permeability studies. Notably, these promising agents exhibited negligible toxicity mammalian red blood cells. Additionally, explored potential 12 active disrupt established biofilms 38. most effective biofilm disruptors were ethyl octyl-naphthyl (10c 10 k). These 10c k disrupted 51 % at 4x (MIC = 17.6 11.2 mL−1) 56 %-58 8x 35.2 22.4 Overall, this research contributes insights design principles activity, implications for development new compounds.

Language: Английский

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Preparation and biological evaluation of coumarin amide derivatives bearing fluorine as potential fungicides and anticancer agents

Arabian Journal of Chemistry, Journal Year: 2024, Volume and Issue: 17(9), P. 105872 - 105872

Published: June 12, 2024

In order to find new potential fungicides and anticancer agents, a series of coumarin amide derivatives bearing fluorine were synthesized characterized spectroscopically. Compounds A6, B11, C2 C7 confirmed by X-ray diffraction further. The antifungal bioassays against five typical pathogenic fungi showed that compound C5 exhibited more remarkable fungicidal activities Alternaria alternata (EC50 = 11.5 μg/mL), Colletotrichum gloeosporioides 18.0 Pyricularia grisea 33.8 surpassing kresoxim-methyl. Molecular docking result indicated displayed high binding affinity chitinase, which plays crucial role in degradation remodeling fungal cell walls. addition, the three cancer cells demonstrated A4 excellent growth inhibitory effect Hela with IC50 value 8.13 μM, low cytotoxicity human normal BEAS-2B. Flow cytometric analysis further significantly arrested cycle at S phase trigger apoptosis. With above interesting biological profile, these could be used as anfungicides candidates.

Language: Английский

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Targeting bacterial phospholipids and their synthesis pathways for antibiotic discovery

Progress in Lipid Research, Journal Year: 2024, Volume and Issue: unknown, P. 101307 - 101307

Published: Nov. 1, 2024

Language: Английский

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