DNA Gyrase as a Target for Quinolones

Biomedicines, Journal Year: 2023, Volume and Issue: 11(2), P. 371 - 371

Published: Jan. 27, 2023

Bacterial DNA gyrase is a type II topoisomerase that can introduce negative supercoils to substrates and clinically-relevant target for the development of new antibacterials. one primary targets quinolones, broad-spectrum antibacterial agents are used as first-line drug various types infections. However, currently quinolones becoming less effective due resistance. Common resistance comes in form mutation enzyme targets, with this being most clinically relevant. Additional mechanisms, conducive quinolone resistance, arbitrated by chromosomal mutations and/or plasmid-gene uptake alter cellular concentration interaction target, or affect metabolism. Significant synthetic strategies have been employed modify scaffold develop novel overcome problem. This review discusses antibiotics targeting bacterial reduce toxicity. Moreover, structural activity relationship (SAR) data included could be useful future generations antibiotics.

Language: Английский

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Recent advancements in the development of heterocyclic anti-inflammatory agents

European Journal of Medicinal Chemistry, Journal Year: 2020, Volume and Issue: 200, P. 112438 - 112438

Published: May 15, 2020

Language: Английский

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1,2,3-Triazole-containing hybrids with potential antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA)

European Journal of Medicinal Chemistry, Journal Year: 2020, Volume and Issue: 206, P. 112686 - 112686

Published: Aug. 5, 2020

Language: Английский

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Recent advances in TiO2-based materials for photocatalytic degradation of antibiotics in aqueous systems

Environmental Technology & Innovation, Journal Year: 2021, Volume and Issue: 24, P. 101822 - 101822

Published: July 28, 2021

Language: Английский

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Structure–Activity Relationship Analysis of Benzimidazoles as Emerging Anti-Inflammatory Agents: An Overview

Pharmaceuticals, Journal Year: 2021, Volume and Issue: 14(7), P. 663 - 663

Published: July 11, 2021

A significant number of the anti-inflammatory drugs currently in use are becoming obsolete. These exceptionally hazardous for long-term because their possible unfavourable impacts. Subsequently, ebb-and-flow decade, analysts and researchers engaged developing new drugs, many such agents later phases clinical trials. Molecules with heterocyclic nuclei similar to various natural antecedents, thus acquiring immense consideration from scientific experts researchers. The arguably most adaptable cores benzimidazoles containing nitrogen a bicyclic scaffold. Numerous benzimidazole broadly used treatment numerous diseases, showing promising therapeutic potential. Benzimidazole derivatives exert effects mainly by interacting transient receptor potential vanilloid-1, cannabinoid receptors, bradykinin specific cytokines, 5-lipoxygenase activating protein cyclooxygenase. Literature on structure–activity relationship (SAR) investigations highlight that substituent’s tendency position ring significantly contribute activity. Reported SAR analyses indicate substitution at N1, C2, C5 C6 positions scaffold greatly influence For example, substituted anacardic acid C2 inhibits COX-2, 5-carboxamide or sulfamoyl sulfonyl antagonises receptor, whereas diarylamine C3 carboxamide result antagonism receptor. In this review, we examine insights regarding SARs compounds, which will be helpful designing target inflammation-promoting enzymes.

Language: Английский

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Identification of Novel Cyanopyridones and Pyrido[2,3-d]Pyrimidines as Anticancer Agents with Dual VEGFR-2/HER-2 Inhibitory Action: Synthesis, Biological Evaluation and Molecular Docking Studies

Pharmaceuticals, Journal Year: 2022, Volume and Issue: 15(10), P. 1262 - 1262

Published: Oct. 13, 2022

In the current work, we designed and synthesized three families of non-fused fused compounds based on cyanopyridone: derivatives 6-amino-1,2-dihydropyridine-3,5-dicarbonitrile (5a-f) 3,4,7,8-tetrahydro pyrimidine-6-carbonitrile (6a-b 7a-e). The newly compounds' structure were determined using a variety techniques, including 1H NMR, 13C mass spectrum, infrared spectroscopy, elemental analysis. developed tested for ability to inhibit growth breast adenocarcinoma (MCF-7) hepatic (HepG2) cell lines MTT assay. Some more effective towards cancer than standard treatment taxol. best antiproliferative activities demonstrated by cyanopyridones 5a 5e against MCF-7 line (IC50 = 1.77 1.39 μM, respectively) 6b HepG2 2.68 2.71 respectively). We further explored 5e, two most potent line, their VEGFR-2 HER-2. Finally, docking molecular dynamics simulations performed as part modeling investigation elucidate binding modes compounds, allowing thorough comprehension activity 5e.

Language: Английский

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Quinolone: a versatile therapeutic compound class

Molecular Diversity, Journal Year: 2022, Volume and Issue: 27(3), P. 1501 - 1526

Published: Dec. 17, 2022

Language: Английский

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New Efforts toward Aminothiazolylquinolones with Multitargeting Antibacterial Potential

Journal of Agricultural and Food Chemistry, Journal Year: 2023, Volume and Issue: 71(5), P. 2322 - 2332

Published: Jan. 26, 2023

New antibacterial 3-(aminothiazolyl)quinolones (ATQs) were designed and efficiently synthesized to counteract the growing multidrug resistance in animal husbandry. Bioactive assays manifested that N,N-dicyclohexylaminocarbonyl ATQ 10e methyl 17a, respectively, showed better behavior against Staphylococcus aureus ATCC 29213 Pseudomonas aeruginosa than reference drug norfloxacin. Notably, highly active 17a with low hemolysis, negligible mammalian cytotoxicity, good pharmacokinetic properties displayed trends induce synergistic combinations Preliminary mechanism exploration implied representative could inhibit formation of biofilms destroy bacterial membrane integrity, further binding intracellular DNA gyrase hinder replication. also production excess reactive oxygen species reduce metabolism accelerate death. These results provided a promise for as new potential multitargeting agents treat infection animals.

Language: Английский

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Recent advances in the synthesis of pharmaceutically active 4-quinolone and its analogues: a review

RSC Advances, Journal Year: 2023, Volume and Issue: 13(13), P. 8657 - 8682

Published: Jan. 1, 2023

4-Quinolone and its analogs are heterocyclic classes of organic compounds displaying biologically active a broad spectrum pharmaceutical drug scaffolds.

Language: Английский

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Navigating Antibacterial Frontiers: A Panoramic Exploration of Antibacterial Landscapes, Resistance Mechanisms, and Emerging Therapeutic Strategies

ACS Infectious Diseases, Journal Year: 2024, Volume and Issue: 10(5), P. 1483 - 1519

Published: May 1, 2024

The development of effective antibacterial solutions has become paramount in maintaining global health this era increasing bacterial threats and rampant antibiotic resistance. Traditional antibiotics have played a significant role combating infections throughout history. However, the emergence novel resistant strains necessitates constant innovation research. We analyzed data on antibacterials from CAS Content Collection, largest human-curated collection published scientific knowledge, which proven valuable for quantitative analysis knowledge. Our focuses mining Collection recent publications (since 2012). This article aims to explore intricate landscape research while reviewing advancement traditional emerging strategies. By delving into resistance mechanisms, paper highlights need find alternate strategies address growing concern.

Language: Английский

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