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Journal ArticleDOI

Development of dilipid polymyxins: Investigation on the effect of hydrophobicity through its fatty acyl component.

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TLDR
An understanding to the polymyxin structure is provided that may be used to usher the development of enhanced polymyXin analogs, suggesting that the lipid component of poly myxin plays an important role in resisting active efflux.
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This article is published in Bioorganic Chemistry.The article was published on 2018-07-19. It has received 13 citations till now. The article focuses on the topics: Polymyxin & Colistin.

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Colistin and its role in the Era of antibiotic resistance: an extended review(2000–2019)

TL;DR: This review intends to discuss the progress over the last two decades in understanding the alternative colistin mechanisms of action and different strategies used by bacteria to develop resistance againstcolistin, besides providing an update about what is previously recognized and what is novel concerning colistsin resistance.
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Chemically modified and conjugated antimicrobial peptides against superbugs.

TL;DR: In this paper, a review summarises recent synthetic efforts and their impact on analogue design as well as their various applications in AMP development, including modifications that have been reported to enhance antimicrobial activity including lipidation, glycosylation and multimerization through to the broad application of novel bio-orthogonal chemistry.
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The Anthelmintic Drug Niclosamide Synergizes with Colistin and Reverses Colistin Resistance in Gram-Negative Bacilli.

TL;DR: It is demonstrated that the anthelmintic drug niclosamide selectively synergized with the lipopeptide antibiotic colistin against colist in-susceptible but more importantly against colistsin-resistant GNB, including clinical isolates that harbor the mcr-1 gene.
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Synergistic combinations of anthelmintic salicylanilides oxyclozanide, rafoxanide, and closantel with colistin eradicates multidrug-resistant colistin-resistant Gram-negative bacilli.

TL;DR: In vitro data corroborate the repositioning of the three salicylanilides as adjuvants to counter resistance to the antibiotic of last resort colistin and are timely and relevant since the global dissemination of plasmid-mediated Colistin resistance had been realized.
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Binding interactions of bacterial lipopolysaccharides to polymyxin B in an amphiphilic carrier ‘sodium deoxycholate sulfate’

TL;DR: The NMR and IR studies showed that the presence of SDCS, the hydrophobicity of PMB increased by hydrogen bonding and electrostatic interactions and formed stabilized PMB-SDCS micelles.
References
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Journal ArticleDOI

Structure—Activity Relationships of Polymyxin Antibiotics

TL;DR: This research presents a novel and scalable approaches that allow for real-time decision-making in the design and implementation of drug 505(b) agonist regimens for the treatment of central nervous system disorders.
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Substrate Specificities of MexAB-OprM, MexCD-OprJ, and MexXY-OprM Efflux Pumps in Pseudomonas aeruginosa

TL;DR: To find the exact substrate specificities of three species of tripartite efflux systems of Pseudomonas aeruginosa, MexAB-OprM, MexCD- oprJ, and MexXY-OPRM, a series of isogenic mutants were constructed, each constitutively overproduced one of the three efflux system and lacked the other two.

Substrate specificities of mexaboprm, mexcd-oprj, and mexxyoprm efflux pumps in pseudomonas aeruginosa

TL;DR: In this article, the exact substrate specificities of three species of tripartite efflux systems of Pseudomonas aeruginosa, MexAB-OprM, MexCD-OplJ, and MexXY-OPRM were found.
Journal ArticleDOI

Defining Fractional Inhibitory Concentration Index Cutoffs for Additive Interactions Based on Self-Drug Additive Combinations, Monte Carlo Simulation Analysis, and In Vitro-In Vivo Correlation Data for Antifungal Drug Combinations against Aspergillus fumigatus

TL;DR: The fractional inhibitory concentration (FIC) index range of 0.5 to 4 that is commonly used to define additivity results in no interactions in most combination studies of antifungal agents, which is reassessed based on experimental variation of the checkerboard technique and in vitro-in vivo correlation.
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