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

ACS Applied Materials & Interfaces, Год журнала: 2025, Номер unknown

Опубликована: Янв. 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

Язык: Английский

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Evaluation of novel compounds as anti-bacterial or anti-virulence agents

Frontiers in Cellular and Infection Microbiology, Год журнала: 2024, Номер 14

Опубликована: Март 6, 2024

Antimicrobial resistance is a global threat, leading to an alarming increase in the prevalence of bacterial infections that can no longer be treated with available antibiotics. The World Health Organization estimates by 2050 up 10 million deaths per year could associated antimicrobial resistance, which would equal annual number cancer worldwide. To overcome this emerging crisis, novel anti-bacterial compounds are urgently needed. There two possible approaches fight against infections: a) targeting structures within cells, similar existing antibiotics; and/or b) virulence factors rather than growth. Here, for first time, we provide comprehensive overview key steps evaluation potential new anti-virulence compounds. methods described review include:

Язык: Английский

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Structure optimizing of flavonoids against both MRSA and VRE

European Journal of Medicinal Chemistry, Год журнала: 2024, Номер 271, С. 116401 - 116401

Опубликована: Апрель 16, 2024

Язык: Английский

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

European Journal of Medicinal Chemistry, Год журнала: 2024, Номер 276, С. 116716 - 116716

Опубликована: Июль 26, 2024

Язык: Английский

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Synthesis and anti-MRSA activity of quaternized small molecule antimicrobial peptide mimics based on norharmane

European Journal of Medicinal Chemistry, Год журнала: 2025, Номер 290, С. 117518 - 117518

Опубликована: Март 14, 2025

Язык: Английский

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Total Synthesis of Auriculatin and Millexatin F and Discovery of Their Antibacterial Mechanism

ACS Omega, Год журнала: 2025, Номер 10(16), С. 16265 - 16276

Опубликована: Апрель 15, 2025

The emergence of multidrug-resistant (MDR) bacteria necessitates the urgent development novel antibacterial agents. This study reported first total synthesis two isoflavones, auriculatin (1) and millexatin F (2), derived from tropical medicinal plant Millettia extensa. Through in vitro evaluations, both compounds 1 2 possessed significant activities (MICs = 0.5-4 μg/mL) rapid bactericidal properties against Gram-positive bacteria, along with high safety for mammalian cells. Mechanistic studies revealed that (2) interact bacterial cell membranes, inducing alterations morphology membrane permeability a rise leakage intracellular DNA proteins, thereby leading to death. In addition, our indicated could phosphatidylethanolamine (PE) cardiolipin (CL) cytoplasmic membranes Gram-negative bacteria. Furthermore, showed increased efficacy when combined permeabilizer (polymyxin B nonapeptide), indicating potential broader application. These findings underscore therapeutic promise as lead candidates fight infections.

Язык: Английский

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Design, Synthesis, and Characterization of Novel Cannabidiol-Based Derivatives with Potent Antioxidant Activities

International Journal of Molecular Sciences, Год журнала: 2024, Номер 25(17), С. 9579 - 9579

Опубликована: Сен. 4, 2024

In recent years, extensive research has focused on cannabidiol (CBD), a well-studied non-psychoactive component of the plant-derived cannabinoids. CBD shown significant therapeutic potential for treating various diseases and disorders, including antioxidants anti-inflammatory effects. Due to promising effect in wide variety diseases, synthetic derivatization this compound attracted attention drug discovery both industry academia. current research, we by introducing Schiff base moieties, particularly (thio)-semicarbazide aminoguanidine motifs, at 3-position olivetolic ring. We have designed, synthesized, characterized new derivatives based CBD’s framework, specifically aminoguanylhydrazone- (thio)-semicarbazones-CBD-aldehyde compounds. Their antioxidant was assessed using FRAP DPPH assays, alongside an evaluation their LDL oxidation induced Cu2+ AAPH. Our findings suggest that incorporating thiosemicarbazide motif into framework produces potent antioxidant, warranting further investigation.

Язык: Английский

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Design, synthesis, and evaluation of pyranochromene derivatives as membrane targeting antibacterials against Gram-positive bacteria

Bioorganic & Medicinal Chemistry Letters, Год журнала: 2024, Номер 113, С. 129949 - 129949

Опубликована: Сен. 6, 2024

Язык: Английский

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Development of membrane-targeting chalcone derivatives as antibacterial agents against multidrug-resistant bacteria

European Journal of Medicinal Chemistry, Год журнала: 2024, Номер 280, С. 116969 - 116969

Опубликована: Окт. 18, 2024

Язык: Английский

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Magnetite graphene oxide incorporated κ-carrageenan/alginate nanobiocomposite for photothermal therapy and multi-stimuli-responsive sunitinib release

Journal of Drug Delivery Science and Technology, Год журнала: 2024, Номер unknown, С. 106576 - 106576

Опубликована: Дек. 1, 2024

Язык: Английский

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