Comprehensive Insights into Medicinal Research on Imidazole-Based Supramolecular Complexes

Pharmaceutics, Год журнала: 2023, Номер 15(5), С. 1348 - 1348

Опубликована: Апрель 27, 2023

The electron-rich five-membered aromatic aza-heterocyclic imidazole, which contains two nitrogen atoms, is an important functional fragment widely present in a large number of biomolecules and medicinal drugs; its unique structure beneficial to easily bind with various inorganic or organic ions molecules through noncovalent interactions form variety supramolecular complexes broad potential, being paid increasing amount attention regarding more contributions imidazole-based for possible application. This work gives systematical comprehensive insights into research on complexes, including anticancer, antibacterial, antifungal, antiparasitic, antidiabetic, antihypertensive, anti-inflammatory aspects as well ion receptors, imaging agents, pathologic probes. new trend the foreseeable near future toward chemistry also prospected. It hoped that this provides help rational design drug agents effective diagnostic pathological

Язык: Английский

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Identification of unique indolylcyanoethylenyl sulfonylanilines as novel structural scaffolds of potential antibacterial agents

European Journal of Medicinal Chemistry, Год журнала: 2023, Номер 260, С. 115773 - 115773

Опубликована: Авг. 30, 2023

Язык: Английский

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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 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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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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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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Discovery of Quinazolone Pyridiniums as Potential Broad-Spectrum Antibacterial Agents

Molecules, Год журнала: 2025, Номер 30(2), С. 243 - 243

Опубликована: Янв. 9, 2025

The overprescription of antibiotics in medicine and agriculture has accelerated the development spread antibiotic resistance bacteria, which severely limits arsenal available to clinicians for treating bacterial infections. This work discovered a new class heteroarylcyanovinyl quinazolones quinazolone pyridiniums surmount increasingly severe resistance. Bioactive assays manifested that highly active compound 19a exhibited strong inhibition against MRSA Escherichia coli with extremely low MICs 0.5 μg/mL, being eightfold more than norfloxacin (MICs = 4 μg/mL). rapid bactericidal properties displayed imperceptible trends, negligible hemolytic toxicity, effective biofilm inhibitory effects. Preliminary explorations on antibacterial mechanisms revealed could cause membrane damage, embed intracellular DNA hinder replication, induce metabolic dysfunction. Surprisingly, was found trigger conformational change PBP2a open site, might account its high MRSA. In addition, little effect molecule production reactive oxygen species indicated death not caused by oxidative stress. above comprehensive analyses highlighted large potential as multitargeting broad-spectrum agents.

Язык: Английский

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A comprehensive insight into naphthalimides as novel structural skeleton of multitargeting promising antibiotics

Future Medicinal Chemistry, Год журнала: 2025, Номер unknown, С. 1 - 16

Опубликована: Фев. 16, 2025

The globally growing antimicrobial resistance seriously threatens human health, increasing efforts have been devoting to the development of novel antibiotics. Naphthalimides contain a special skeleton cyclic double imides and naphthalene framework, this unique structure can exert multitargeting abilities which are helpful overcome escalating issue resistance. Therefore, research in connection with naphthalimides as agents is becoming progressively active. It has revealed that structural promising antibiotics could not only target DNAs enzymes, disturb membrane, produce reactive oxygen species, etc. suggesting actions do induce resistance, but also show broad spectrum safety profile pharmacokinetic characteristics, implying large potential new type via continuous toward naphthalimides. This review presents discusses rational design strategies, structure-activity relationships, mechanisms action, comprehensive view providing insight for efficient, broad-spectrum, low-toxic naphthalimide

Язык: Английский

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Benzo-α-pyrone-derived multitargeting actions to enhance the antibacterial performance of sulfanilamides against Escherichia coli

Bioorganic Chemistry, Год журнала: 2025, Номер 158, С. 108339 - 108339

Опубликована: Март 5, 2025

Язык: Английский

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