Design, synthesis and antibacterial evaluation of a novel class of tetrahydrobenzothiophene derivatives

Lai, Lin; Yang, Jinhua; Sun, Wanlin; Su, Xin; Chen, Xinan; Pei, Shuchen

doi:10.1039/d2md00373b

Cited by 4 publications

(2 citation statements)

References 29 publications

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“…One candidate showed MIC values of 1.1 µM against E. coli, 1.0 µM against P. aeruginosa, 0.5 µM against Salmonella, and 1.1 µM against S. aureus. This demonstrates a promising lead compound for the development of new antimicrobial agents against MDR and persistent bacteria [42,43]. Recently, the biological effects of verapamil, an inhibitor of ABC transporters, were investigated in P. aeruginosa.…”

Section: Lps Transportmentioning

confidence: 99%

Advances in Development of Novel Therapeutic Strategies against Multi-Drug Resistant Pseudomonas aeruginosa

Yin,

Alam,

Fallon

et al. 2024

Antibiotics

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Pseudomonas aeruginosa (P. aeruginosa) with multi-drug resistance (MDR) is a major cause of serious healthcare-associated infections, leading to high morbidity and mortality. This opportunistic pathogen is responsible for various infectious diseases, such as those seen in cystic fibrosis, ventilator-associated pneumonia, urinary tract infection, otitis externa, and burn and wound injuries. Due to its relatively large genome, P. aeruginosa has great diversity and can use various molecular mechanisms for antimicrobial resistance. For example, outer membrane permeability can contribute to antimicrobial resistance and is determined by lipopolysaccharide (LPS) and porin proteins. Recent findings on the regulatory interaction between peptidoglycan and LPS synthesis provide additional clues against pathogenic P. aeruginosa. This review focuses on recent advances in antimicrobial agents and inhibitors targeting LPS and porin proteins. In addition, we explore current and emerging treatment strategies for MDR P. aeruginosa, including phages, vaccines, nanoparticles, and their combinatorial therapies. Novel strategies and their corresponding therapeutic agents are urgently needed for combating MDR pathogens.

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Section: Lps Transportmentioning

confidence: 99%

Advances in Development of Novel Therapeutic Strategies against Multi-Drug Resistant Pseudomonas aeruginosa

Yin,

Alam,

Fallon

et al. 2024

Antibiotics

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“…In addition, positively charged water-soluble IPECs will contain charge-compensated regions, which will improve adhesion on hydrophobic surfaces. However, it is known that, in general, polycations have lower biocidal activity compared to low-molecular-weight bioactive compounds [ 20 , 21 , 22 , 23 , 24 , 25 , 26 ]. In this regard, modifying IPEC by including an additional low-molecular-weight biocidal agent, for example, metal nano particles or metal oxides, is proposed.…”

Section: Introductionmentioning

confidence: 99%

Ag2O-Containing Biocidal Interpolyelectrolyte Complexes on Glass Surfaces—Adhesive Properties of the Coatings

Pigareva,

Paltsev,

Marina

et al. 2023

Polymers

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Biocidal coatings are of great interest to the healthcare system. In this work, the biocidal activity of coatings based on a complex biocide containing polymer and inorganic active antibacterial components was studied. Silver oxide was distributed in a matrix of a positively charged interpolyelectrolyte complex (IPEC) of polydiallyldimethylammonium chloride (PDADMAC) and sodium polystyrene sulfonate (PSS) using ultrasonic dispersion, forming nanoparticles with an average size of 5–6 nm. The formed nanoparticles in the matrix are not subject to agglomeration and changes in morphology during storage. It was found that the inclusion of silver oxide in a positively charged IPEC allows a more than 4-fold increase in the effectiveness of the complex biocide against E. coli K12 in comparison with the biocidal effect of PDADMAC and IPEC. Polycation, IPEC, and the IPEC/Ag2O ternary complex form coatings on the glass surface due to electrostatic adsorption. Adhesive and cohesive forces in the resulting coatings were studied with micron-scale coatings using dynamometry. It was found that the stability of the coating is determined primarily by adhesive interactions. At the macro level, it is not possible to reliably identify the role of IPEC formation in adhesion. On the other hand, use of the optical tweezers method makes it possible to analyze macromolecules at the submicron scale and to evaluate the multiple increase in adhesive forces when forming a coating from IPEC compared to coatings from PDADMAC. Thus, the application of ternary IPEC/Ag2O complexes makes it possible to obtain coatings with increased antibacterial action and improved adhesive characteristics.

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Discovery of novel tetrahydrobenzothiophene derivatives as MSBA inhibitors for antimicrobial agents

Pei,

Lai,

Sun

et al. 2024

Bioorganic Chemistry

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Design, synthesis and antibacterial evaluation of a novel class of tetrahydrobenzothiophene derivatives

Abstract: In this study, a new series of tetrahydrobenzothiophene derivatives have been designed.

Cited by 4 publications

References 29 publications

Advances in Development of Novel Therapeutic Strategies against Multi-Drug Resistant Pseudomonas aeruginosa

Advances in Development of Novel Therapeutic Strategies against Multi-Drug Resistant Pseudomonas aeruginosa

Ag2O-Containing Biocidal Interpolyelectrolyte Complexes on Glass Surfaces—Adhesive Properties of the Coatings

Discovery of novel tetrahydrobenzothiophene derivatives as MSBA inhibitors for antimicrobial agents

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