Novel aminothiazoximone-corbelled ethoxycarbonylpyrimidones with antibiofilm activity to conquer Gram-negative bacteria through potential multitargeting effects

European Journal of Medicinal Chemistry, Год журнала: 2024, Номер 268, С. 116219 - 116219

Опубликована: Фев. 13, 2024

Язык: Английский

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Cyanomethylquinolones as a New Class of Potential Multitargeting Broad-Spectrum Antibacterial Agents

Journal of Medicinal Chemistry, Год журнала: 2024, Номер 67(11), С. 9028 - 9053

Опубликована: Май 24, 2024

This work identified a class of cyanomethylquinolones (CQs) and their carboxyl analogues as potential multitargeting antibacterial candidates. Most the prepared compounds showed high activities against most tested bacteria, exhibiting lower MIC values (0.125–2 μg/mL) than those clinical norfloxacin, ciprofloxacin, clinafloxacin. The low hemolysis, drug resistance, cytotoxicity, well good predictive pharmacokinetics active CQs revealed development potential. Furthermore, they could eradicate established biofilm, facilitating bacterial exposure to these These induce death through effects, including intercalating into DNA, up-regulating reactive oxygen species, damaging membranes directly, impeding metabolism. Moreover, highly cyclopropyl CQ 15 exhibited more effective in vivo anti-MRSA potency ciprofloxacin. findings highlight broad-spectrum candidates for treating intractable infections.

Язык: Английский

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Unique Azolyl Acylhydrazonyl Hybridization of Aloe Emodins to Access Potential Antibacterial Agents

Chinese Journal of Chemistry, Год журнала: 2024, Номер 42(15), С. 1741 - 1758

Опубликована: Март 26, 2024

Comprehensive Summary A type of unique azole‐hybridized acylhydrazonyl aloe emodins (AAEs) were developed as new antibacterial agents for combating bacterial infections. Some target AAEs showed strong activities, especially, tetrazolylthioether AAE 27a exhibited broad spectrum with 16—256 folds and 8—64 more active efficacy than the reference drugs emodin norfloxacin, respectively. Tetrazolylthioether also gave low hemolysis cytotoxicity, well favorable bioavailability. Preliminary mechanism explorations revealed that could cause membrane depolarization damage cell membrane, resulting in nucleic acid leakage. Moreover, compound intercalate into DNA to impede its replication form supramolecular ‐DNA gyrase complex disturb function gyrase. These findings would provide valuable insights further exploration azolyl potential candidates.

Язык: Английский

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Hydrazyl hydroxycoumarins as new potential conquerors towards Pseudomonas aeruginosa

Bioorganic & Medicinal Chemistry Letters, Год журнала: 2024, Номер 103, С. 129709 - 129709

Опубликована: Март 15, 2024

Язык: Английский

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Unique aminothiazolyl coumarins as potential DNA and membrane disruptors towards Enterococcus faecalis

Bioorganic Chemistry, Год журнала: 2024, Номер 148, С. 107451 - 107451

Опубликована: Май 13, 2024

Язык: Английский

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Discovery of indolylacryloyl-derived oxacins as novel potential broad-spectrum antibacterial candidates

European Journal of Medicinal Chemistry, Год журнала: 2024, Номер 270, С. 116392 - 116392

Опубликована: Апрель 1, 2024

Язык: Английский

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A Unique Hybridization Route to Access Hydrazylnaphthalimidols as Novel Structural Scaffolds of Multitargeting Broad-Spectrum Antifungal Candidates

Journal of Medicinal Chemistry, Год журнала: 2024, Номер 67(11), С. 8932 - 8961

Опубликована: Май 30, 2024

This study developed a class of novel structural antifungal hydrazylnaphthalimidols (HNs) with multitargeting broad-spectrum potential

Язык: Английский

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Discovery of benzopyridone cyanoacetates as new type of potential broad-spectrum antibacterial candidates

European Journal of Medicinal Chemistry, Год журнала: 2023, Номер 265, С. 116107 - 116107

Опубликована: Дек. 30, 2023

Язык: Английский

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Synthesis and antibacterial medicinal evaluation of carbothioamido hydrazonyl thiazolylquinolone with multitargeting antimicrobial potential to combat increasingly global resistance

European Journal of Medicinal Chemistry, Год журнала: 2024, Номер 275, С. 116626 - 116626

Опубликована: Июнь 27, 2024

Язык: Английский

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Synthesis and Antimicrobial Evaluation of Novel Quaternary Quinolone Derivatives with Low Toxicity and Anti-Biofilm Activity

Опубликована: Янв. 1, 2025

Язык: Английский

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