5-Benzylidene-4-Oxazolidinones Are Synergistic with Antibiotics for the Treatment of Staphylococcus aureus Biofilms

The failure of frontline antibiotics in the clinic is one of the most serious threats to human health and requires a multitude of novel therapeutics and innovative approaches to treatment so as to curtail the growing crisis. In addition to traditional resistance mechanisms resulting in the lack of efficacy of many antibiotics, most chronic and recurring infections are further made tolerant to antibiotic action by the presence of biofilms. Herein, we report an expanded set of 5-benzylidene-4-oxazolidinones that are able to inhibit the formation of Staphylococcus aureus biofilms, disperse preformed biofilms, and, in combination with common antibiotics, are able to significantly reduce the bacterial load in a robust collagen-matrix model of biofilm infection.     

Biocatalytic Alkylation Cascades: Recent Advances and Future Opportunities for Late-Stage Functionalization

This Concept article describes the latest developments in the emerging area of late-stage biocatalytic alkylation. Central to these developments is the ability to efficiently prepare S-adenosyl methionine (SAM) cofactor analogues and couple this with enzymatic alkyl transfer. Recent developments in the enzymatic synthesis of SAM cofactor analogues are summarized first, followed by their application as alkyl transfer agents catalyzed by methyltransferases (MTases). Second, innovative methods to regenerate SAM cofactors by enzymatic cascades is reported. Finally, future opportunities towards establishing a generalized platform for late-stage alkylation are described.     

Activity-Directed Synthesis: A Flexible Approach for Lead Generation

Activity-directed synthesis (ADS) is a structure-blind, functional-driven molecular discovery approach. In this Concept, four case studies highlight the general applicability of ADS and showcase its flexibility to support different medicinal chemistry strategies. ADS deliberately harnesses reactions with multiple possible outcomes, and allows many chemotypes to be evaluated in parallel. Resources are focused on bioactive molecules, which emerge in tandem with associated synthetic routes. Some of the future challenges for ADS are highlighted, including the realisation of an autonomous molecular discovery platform. The prospects for ADS to become a mainstream lead generation approach are discussed.     

Potentiometric sensors with plastized poly(vinyl chloride) membranes selective to penicillin antibiotics: Properties and applications

Potentiometric sensors with plasticized poly(vinyl chloride) membranes based on β-lactam–tetraalkylammonium ion associates sensitive to penicillin antibiotics are proposed. The physicochemical characteristics (solubility product constants and dissociation constants) of active membrane components and the electrode, transport, and selective properties of the membranes of liquidand solid-contact sensors have been studied. The quantitative characteristics of membrane transport (penetrability, ion flux, and transport rate) have been evaluated. The main charge carriers in the membranes and at the membrane/solution interface have been determined from the membrane transport characteristics. The potentiometric sensors are shown to be applicable to the determination of penicillin antibiotics in biological fluids (blood serum and oral fluid) from patients with urinary tract infection.     

Effect of Boronizing on Operating Stability of Steel AISI 304L under Erosion Impact of Hard Particles

Metal Science and Heat Treatment - The effect of solid boronizing at 950°C for 2 and 4 h on the phase composition, microstructure, hardness and abrasive wear of steel AISI 304L is studied...     

Flexible poly(styrene-ethylene-butadiene-styrene) hybrid nanofibers for bioengineering and water filtration applications

Among the thermoplastic elastomers that play important roles in the polymer industry due to their superior properties, styrene-based species and polyurethane block copolymers are of great interest. Poly(styrene-ethylene-butadiene-styrene) (SEBS) as a triblock copolymer seems to have the potential to meet many demands in different applications due to various industrial requirements where durability, biocompatibility, breaking elongation, and interfacial adhesion are important. In this study, the SEBS triblock copolymer was functionalized with natural (Satureja hortensis, SH) and synthetic (nanopowder, TiO₂) agents to obtain composite nanofibers by electrospinning and electrospraying methods for use in biomedical and water filtration applications. The results were compared with thermoplastic polyurethane (TPU) composite nanofibers, which are commonly used in these fields. Here, functionalized SEBS nanofibers exhibited antibacterial effect while at the same time improving cell viability. In addition, because of successful water filtration by using the SEBS composite nanofibers, the material may have a good potential to be used comparably to TPU for the application.