Recent Updates on Antibacterial Quinolones: Green Synthesis, Mode of Interaction and Structure–Activity Relationship

Chemistry & Biodiversity, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 5, 2025

ABSTRACT Quinolone antibiotics are a crucial class of synthetic antibacterial agents, widely utilized due to their broad spectrum activity. Due the development antimicrobial resistance, potency quinolone drugs decreased. Many conventional methods have been developed elevate amination rate and improve yield. These generally characterized by prolonged reaction durations, high boiling solvents, harsh conditions, costly reagents excessive heat generation, which adversely affected therapeutic efficacy these compounds. Recently, green chemistry has focused on sustainable chemistry‐dependent analogue synthesis that significantly reduce bacterial infections. include one‐pot synthesis, photoredox catalysis, phase transfer ultrasonic irradiation, microwave‐assisted, solvent catalyst‐free often utilize energy‐efficient, non‐toxic less time‐consuming techniques, aligning with principles safety environmental impact. Researchers continuously explore innovative approaches applying in reactions. This review includes comprehensive analysis literature from past 15 years Scopus, PubMed, Embase WOS using keywords, such as chemistry, antibacterial, highlighting significant advancements emerging trends. work's importance lies its extensive overview for quinolones related heterocyclic Furthermore, provide useful information generation future drugs, some structural–activity relationship studies silico also included investigate stable binding interactions between leads various target proteins.

Language: Английский

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Design, Synthesis, and In Silico Studies of New Norfloxacin Analogues with Broad Spectrum Antibacterial Activity via Topoisomerase II Inhibition

Pharmaceuticals, Journal Year: 2025, Volume and Issue: 18(4), P. 545 - 545

Published: April 8, 2025

Background: Novel norfloxacin derivatives were synthesized, characterized, and screened for their antibacterial activity against Gram-positive strain S. aureus ATCC 6538 Gram-negative strains; E. coli 25923, K. pneumoniae 10031, P. aeruginosa 27853 using the agar cup diffusion method. Results: The results revealed that compounds 6–17 exhibited more potent towards with MIC values of 0.21–3.61 µM than a 7.83 µM. most compound, 6, showed 37-fold potency norfloxacin. More importantly, compound 7 MRSA norfloxacin, 0.80 1.96 µM, respectively. Meanwhile, 15 16 have strains 0.20–0.79 compared 0.24 Moreover, higher topoisomerase II enzymes, especially IV, which confirms docking study gyrase enzyme active binding site (PDB ID: 2XCT). In addition, cytotoxicity assays 7, 15, negligible risks toxic effects when evaluated normal cell line WI 38. Conclusions: on (PDB: 2XCT) aligns inhibition. physicochemical pharmacokinetic characteristics target forecasted via SwissADME. Hence, these are considered promising candidates require further optimization.

Language: Английский

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Investigation of bacterial DNA gyrase Inhibitor classification models and structural requirements utilizing multiple machine learning methods

Molecular Diversity, Journal Year: 2024, Volume and Issue: 28(4), P. 2119 - 2133

Published: Feb. 19, 2024

Language: Английский

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