Combinatorial and high throughput (HTP) methodologies have long been used by the pharmaceutical industry to accelerate the rate of drug discovery. HTP techniques can also be applied in polymer chemistry to more efficiently elucidate structure−property relationships, to increase the speed of new material development, and to rapidly optimize polymerization conditions. Controlled living/radical polymerization (CLRP) is widely employed in the preparation of potential materials for bioapplications being suitable for a large variety of polymeric materials with various architectures. The versatility of CLRP makes it an ideal candidate for combinatorial and HTP approaches to research, and recently, the development of oxygen tolerant CLRP techniques has greatly simplified the methodology. In this Perspective, we provide an overview of conventional CLRP, including automated parallel synthesizers, as well as oxygen tolerant CLRP applications for HTP polymer research.
The growing trend in antimicrobial resistance is a potential threat to our society. Due to this, the development of new antimicrobial compounds is urgently required. High-throughput compositional analysis, combined with recent advances in polymerization protocols, allows for rapid production of potentially antimicrobial compounds with minimal expertise. This can provide the impetus for correlating activity with composition and functionality. In this study, we have used high-throughput photoinduced electron transfer-reversible addition-fragmentation chain transfer (PET-RAFT) polymerization to test the combinations of seven different monomers using 120 different formulations against three distinct bacterial species: Gram-negative Pseudomonas aeruginosa, Gram-positive Staphylococcus aureus, and Mycobacterium smegmatis. Through variations in composition, we have demonstrated the potential of high-throughput PET-RAFT for highly reproducible products, as well as simultaneous testing of multiple variables. Results indicate that primary amines work best against Gram-negative P. aeruginosa, while quaternary ammonium provides activity versus M. smegmatis. Copolymers of these provide avenues for further optimization, especially in the case of quaternary ammonium functionalities.
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