Synthesis of Novel α-Carboxylate-β-Bismethylsulfanyl Pyrazolyl Schiff Base Derivatives: Targeting DNA gyrase in Antibacterial activity

Journal of Molecular Structure, Год журнала: 2025, Номер unknown, С. 141954 - 141954

Опубликована: Март 1, 2025

Язык: Английский

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Stereoselective synthesis and antibacterial potential of C-3 chloro β-lactams: Insights into DNA gyrase inhibition using in silico molecular docking

International Journal of Biological Macromolecules, Год журнала: 2025, Номер unknown, С. 142713 - 142713

Опубликована: Март 1, 2025

Язык: Английский

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Synthesis, crystal structure, and anticancer activity of organotin(IV) complexes based on chlorine substituted aryl ligands

Medicinal Chemistry Research, Год журнала: 2025, Номер unknown

Опубликована: Фев. 4, 2025

Язык: Английский

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Design, Synthesis and Biological Evaluation of C3‐Indolyl/(3‐chloro‐indolyl)‐C4‐aryl/heteroaryl‐azetidin‐2‐ones

ChemMedChem, Год журнала: 2024, Номер 19(17)

Опубликована: Май 31, 2024

Abstract Herein, trans‐ and cis‐ azetidin‐2‐ones 3–6 were strategically synthesized, capitalizing on the bioactivity of indole pharmacophore, followed by a comprehensive characterization using diverse array spectroscopic techniques. The sixteen examined for antimicrobial activities against both Gram‐negative ( P. aeruginosa , E. coli A. baumannii ) Gram‐positive bacteria (S . aureus, faecium, B. cereus ), as well C. albicans tropicalis fungal strains. highly potent compounds 5 6 b d demonstrated maximum inhibition all multidrug‐resistant strains, with minimum inhibitory concentrations ranging from 0.97–3.9 μg/mL, surpassing potency standard ampicillin (MIC: 3.12–50 μg/mL). Moreover, exhibited significant effects 0.97 μg/mL), comparable to fluconazole. presence C3 ‐(3‐chloro‐indolyl) scaffold, combined electronic at N1/C4 ‐centers, particularly inclusion thiophen‐2‐yl motif, greatly influenced activity target compounds. Assessment 4 i–k THLE‐2 cell lines revealed their preferential safety. Molecular docking studies seven active dual targeting DNA GyrB PBP2a proteins, demonstrating broad‐spectrum antibacterial effect. In silico ADME analysis affirms positive drug‐likeness favorable pharmacokinetic characteristics indole‐derived hybrids, indicating promising potential addressing challenges in evolving multidrug resistance.

Язык: Английский

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Recent progress in synthetic strategies for novel β-lactams linked with five-membered heterocycles (N/O/S): advances in medicinal chemistry (2020–2025)

Medicinal Chemistry Research, Год журнала: 2025, Номер unknown

Опубликована: Апрель 12, 2025

Язык: Английский

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An insights into structural diversity of β-lactam scaffold towards varied medicinal applications: A comprehensive update (2020–2024)

Tetrahedron Letters, Год журнала: 2024, Номер 153, С. 155383 - 155383

Опубликована: Ноя. 16, 2024

Язык: Английский

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Emerging Trends in Microwave and Ultrasound/Visible Light/ Carbene Intermediates & Carbonylation/Metal-Catalyzed Mediated Synthesis of β-Lactams (2021-2024)

Tetrahedron, Год журнала: 2024, Номер unknown, С. 134429 - 134429

Опубликована: Дек. 1, 2024

Язык: Английский

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SYNTHESIS OF NEW IMINE COMPOUNDS BEARING INDOLE AND 1,3,4-THIADIAZOLE MOIETIES: SPECTRAL PROPERTIES, DFT STUDIES, TAUTOMERISM AND BOND ANALYSIS

Journal of Molecular Structure, Год журнала: 2024, Номер unknown, С. 140901 - 140901

Опубликована: Ноя. 1, 2024

Язык: Английский

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