Design, synthesis and biological evaluation of 4-(alkyloxy)-6-methyl-2H-pyran-2-one derivatives as quorum sensing inhibitors

Park, Suzie; Kim, Han Shin; Ok, Kiwon; Kim, Yunhye; Park, Hee Deung; Byun, Youngjoo

doi:10.1016/j.bmcl.2015.05.054

Cited by 40 publications

(21 citation statements)

References 37 publications

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“…Furthermore, they modified the benzo-apyrone scaffold with suitable substitutions, then synthesised and evaluated these compounds fort heir inhibitory activity against BRAF V600E and several melanoma cell lines. [20] In 2015, Mishrae tal. [17] Wu et al,in2016, reported the synthesis and biological evaluation of matrine derivatives built aroundabenzo-a-pyrone scaffold as potent anti-lung-cancer agents.…”

Section: 2 Pharmacological Profile Of Pyrone Derivativesmentioning

confidence: 99%

“…Further analysisb yd ocking revealed that the most potent compound binds to the active site of LasR in amanner similar to the co-crystallised ligand. [20] In 2015, Mishrae tal. reported as eries of 4-oxycoumarin derivatives, ac lass of pyrone, and their evaluation for in vitro and in vivo antifilarial activity against the humanl ymphatic filarial parasite Brugia malayi.…”

Section: Pharmacological Profile Of Pyrone Derivativesmentioning

confidence: 99%

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The Current Status of O‐Heterocycles: A Synthetic and Medicinal Overview

Singh

Silakari

2018

ChemMedChem

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O-Heterocycles have been explored in the field of medicinal chemistry for a long time, but their significance has not been duly recognised and they are often shunned in favour of N-heterocycles. The design of bioactive molecules for nearly every pathophysiological condition is primarily focused on novel N-heterocycles. The main reasons for such bias include the ease of synthesis and possible mimicking of physiological molecules by N-heterocycles. But considering only this criterion rarely provides breakthrough molecules for a given disease condition, and instead the risks of toxicity or side effects are increased with such molecules. On the other hand, owing to improved synthetic feasibility, O-heterocycles have established themselves as equally potent lead molecules for a wide range of pathophysiological conditions. In the last decade there have been hundreds of reports validating the fact that equally potent molecules can be designed and developed by using O-heterocycles, and these are also expected to have comparably low toxicity. Even so, researchers tend to remain biased toward the use of N-heterocycles over O-heterocycles. Thus, this review provides a critical analysis of the synthesis and medicinal attributes of O-heterocycles, such as pyrones, oxazolones, furanones, oxetanes, oxazolidinones, and dioxolonones, and others, reported in the last five years, underlining the need for and the advantages guiding researchers toward them.

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Section: 2 Pharmacological Profile Of Pyrone Derivativesmentioning

confidence: 99%

Section: Pharmacological Profile Of Pyrone Derivativesmentioning

confidence: 99%

The Current Status of O‐Heterocycles: A Synthetic and Medicinal Overview

Singh

Silakari

2018

ChemMedChem

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“…Other furanone analogs have been developed including S-phenyl-l-cysteine sulfoxide and diphenyl disulfide [66] and tetrazole derivatives [67]. Furthermore, synthetic LasR derivatives have been developed such as indole derivatives, non-AHL-like antagonists [68], the synthesized azines derivatives, 4-(alkyloxy)-6-methyl-2H-pyran-2-one [69] and aspirin [70]. Triphenyl hybridγ-butyrolactones and cyclopentanones derivatives are potent inhibitors of LuxR [71].…”

Section: Elimination Of the Qs Signal-receptor Interactionmentioning

confidence: 99%

New Approaches for Competing Microbial Resistance and Virulence

El-Mowafy¹,

Elgaml²,

Shaaban³

2020

Microorganisms

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The spread of multidrug-resistant pathogens together with the development of fatal cases of infectious microorganisms is on the rise. Therefore, there must be new approaches for combating pathogenic microorganisms, either by overcoming antibiotic resistance or via inhibiting their virulence factors. Several virulence factors extremely increase the antimicrobial resistance of various species of pathogens; as a result, the screening of antivirulence agents has gained more and more attention recently. In this aspect, non-traditional strategies that are considered promising in overcoming virulence and pathogenicity of microorganisms will be discussed including; quorum sensing inhibition, antibiofilm, control of the global regulators, bacteriocins and bacteriophages. Applying these methods could provide innovative approaches for competing microbial resistance and virulence.

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“…(Smith et al 2003a). Furthermore, substances blocking regulators of AHL synthesis were identified (Park et al 2015;Soheili et al 2015;Lu et al, 2014a,b). Grampositive bacteria such as S. aureus produce autoinducing peptides that require cleaving for activation and recognition.…”

Section: Page 7 Ofmentioning

confidence: 99%

Anti-virulence Strategies to Target Bacterial Infections

Mühlen

Dersch

2015

Current Topics in Microbiology and Immunology

143

139

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Resistance of important bacterial pathogens to common antimicrobial therapies and the emergence of multidrug-resistant bacteria is increasing at an alarming rate and constitutes one of our greatest challenges in the combat of bacterial infection and accompanied diseases. Given the current shortage of effective drugs, lack of successful prevention measures and only a few new antibiotics in the clinical pipeline demands the development of novel treatment options and alternative antimicrobial therapies. Our increasing understanding of bacterial virulence strategies and the induced molecular pathways of the infectious disease provide novel opportunities to target and interfere with crucial pathogenicity factors or virulence-associated traits of the bacteria while bypassing the evolutionary pressure on the bacterium to develop resistance. In the past decade, numerous new bacterial targets for anti-virulence therapies have been identified, and structure-based tailoring of intervention strategies as well as screening assays for small molecule inhibitors of such pathways were successfully established. In this chapter, we will take a closer look at the bacterial virulence-related factors and processes that present promising targets for antivirulence therapies, recently discovered inhibitory substances and their promises and discuss the challenges and problems that have to be faced.

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Design, synthesis and biological evaluation of 4-(alkyloxy)-6-methyl-2H-pyran-2-one derivatives as quorum sensing inhibitors

Cited by 40 publications

References 37 publications

The Current Status of O‐Heterocycles: A Synthetic and Medicinal Overview

The Current Status of O‐Heterocycles: A Synthetic and Medicinal Overview

New Approaches for Competing Microbial Resistance and Virulence

Anti-virulence Strategies to Target Bacterial Infections

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