Biofilm inhibition of linezolid-like Schiff bases: Synthesis, biological activity, molecular docking and in silico ADME prediction

Sangshetti, Jaiprakash N.; Khan, Firoz A. Kalam; Patil, Rajendra; Marathe, Sayali D.; Gade, W. N.; Shinde, Devanand B.

doi:10.1016/j.bmcl.2014.12.063

Cited by 27 publications

(12 citation statements)

References 43 publications

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“…[39] ChemMedChem 2017, 12,420 -425 www.chemmedchem.org agents. [40] In particular,c ompounds 30 and 31 exhibitedg ood biofilm inhibitory activity,w ith respective IC 50 values of 12.9 and 15.6 mm against P. aeruginosa,m ore active than standard linezolid. SAR studies revealed that the compounds exert varied biofilm inhibitory activity depending on the substituents on aromatic ring.…”

Section: Othersmentioning

confidence: 94%

Recent Advances in the Discovery of PqsD Inhibitors as Antimicrobial Agents

Zhou

2017

ChemMedChem

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The treatment of the infections caused by Pseudomonas aeruginosa, an opportunistic Gram-negative bacterium, is very difficult. High intrinsic tolerance toward common antibiotics and the development of new resistant strains challenge us to find a new treatment as soon as possible. PqsD is an enzyme essential for the P. aeruginosa quorum-sensing apparatus, which catalyzes the final and key step in the biosynthesis of 4-hydroxy-2-heptylquinolone (HHQ), which is a signal molecule of the P. aeruginosa quorum-sensing system. In this review, following an outline on their structures, we present a brief introduction of the PqsD inhibitors including their mechanisms of action, inhibitory activity, and structure-activity relationships.

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Section: Othersmentioning

confidence: 94%

Recent Advances in the Discovery of PqsD Inhibitors as Antimicrobial Agents

Zhou

2017

ChemMedChem

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“…Finally, Sangshetti et al reported the discovery of linezolid-like Schiff bases, which showed promising anti-biofilm activity in the double-digit micromolar range [ 63 ]. Notably, their potency in attenuating biofilm formation was more pronounced than ciprofloxacin and linezolid itself.…”

Section: Reviewmentioning

confidence: 99%

Targeting the Pseudomonas quinolone signal quorum sensing system for the discovery of novel anti-infective pathoblockers

Schütz

Empting

2018

Beilstein J. Org. Chem.

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The Gram-negative opportunistic pathogen Pseudomonas aeruginosa causes severe nosocomial infections. It uses quorum sensing (QS) to regulate and coordinate population-wide group behaviours in the infection process like concerted secretion of virulence factors. One very important signalling network is the Pseudomonas quinolone signal (PQS) QS. With the aim to devise novel and innovative anti-infectives, inhibitors have been designed to address the various potential drug targets present within pqs QS. These range from enzymes within the biosynthesis cascade of the signal molecules PqsABCDE to the receptor of these autoinducers PqsR (MvfR). This review shortly introduces P. aeruginosa and its pathogenicity traits regulated by the pqs system and highlights the published drug discovery efforts providing insights into the compound binding modes if available. Furthermore, suitability of the individual targets for pathoblocker design is discussed.

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“…Drug discovery is a time-consuming, expensive, and interdisciplinary process whereas advances in computational techniques and hardware solutions have enabled in silico methods to speed up lead optimization and identification 8 . ADME screening was carried out in order to understand the pharmacokinetic behaviour of reported derivatives using descriptors like human intestinal absorption (HIA), Lipinski rule of five, blood brain barrier (BBB) penetration, hepatotoxicity, aqueous solubility and inhibition probabilities 9 .…”

Section: Fig 2: Docking Of Anethole With Poly Fig 4: Docking Of Anementioning

confidence: 99%

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2018

IJPSR

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Triple negative breast cancer (TNBC) is a type of breast cancer in which receptors such as estrogen receptor, progesterone receptor, and human epidermal growth factor receptor 2 are absent. Triple-negative breast cancer is a high risk breast cancer that lacks the benefit of specific therapy that targets these receptors. In the present study, anethole an aromatic compound from star anise was exposed to TNBC cell line MDA-MB-231 to assess its anticancer property. Cytotoxicity assay was done to determine and optimize the dose. DNA damage was analyzed by DNA fragmentation method. The use of targeted agents against TNBC such as poly-ADP-ribose and insulin like growth factor receptor were investigated in the present study. The drugtarget interaction was investigated using in-silico docking studies. The insilico study provides evidence for the interaction of anethole with the target proteins namely poly ADP-ribose polymerase (PARP) and insulin like growth factor receptor (IGFIR). This interaction is presumably vital in exerting the anticancerous activity. The present study clearly elucidates that anethole possesses anticancer activity against the TNBC.

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Biofilm inhibition of linezolid-like Schiff bases: Synthesis, biological activity, molecular docking and in silico ADME prediction

Cited by 27 publications

References 43 publications

Recent Advances in the Discovery of PqsD Inhibitors as Antimicrobial Agents

Recent Advances in the Discovery of PqsD Inhibitors as Antimicrobial Agents

Targeting the Pseudomonas quinolone signal quorum sensing system for the discovery of novel anti-infective pathoblockers

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