P. Padnya, Xin Wu, A. Erxleben
Jul 8, 2021
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Influential Citations
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Journal
Frontiers in Chemistry
Abstract
The search for new biologically active compounds to tackle global health challenges is an important goal in organic synthesis, biochemistry, and medicine. The biological activity of macrocyclic structures is an actively developing area of science. Macrocyclic compounds have unique physicochemical properties, such as spatial preorganization, presence of a size-defined cavity, propensity of undergoing self-assembly, low pharmacologically active concentrations, low toxicity, antiallergenicity, etc. Macrocyclic compounds such as crown ethers, cyclodextrins, cucurbiturils, calixarenes, porphyrins, pillararenes and cyclic peptides have been used in various biomedical applications. In this Research Topic, we present a collection of original research and review articles that show the significant recent advances made in the synthesis of new macrocycles and their biomedical applications. One of the ways to overcome the antimicrobial resistance of microorganisms is the use of macrocycle-antibiotic hybrids, as reviewed by Surur et al.. This review article describes the synthesis and properties of the most well-known hybrids of macrocyclic compounds with antibiotics such as rifamycins, vancomycin, etc. It is known that the major limitation of the use of antibiotic hybrids is the increase in molecular weight. However, progresses and advances in this area show the possibility of improving the oral bioavailability of bulky molecules for systemic clinical use. Ibrahim et al. have developed novel Tröger’s base derivatives and studied their anticancer properties. The synthesized Tröger’s base phenhomazines derivatives were screened for anticancer activity, and 1,4,7,10-tetraoxa[10](2,8) trögerophane has shown a promising selectivity on a colon cell line with IC50 92.7 μg/ml. The obtained results open up prospects for the development of new promising anticancer agents. It is known that macrocyclic compounds can be used in targeted delivery systems as containers for drugs. It has been shown by Chandra et al. that cucurbit[7]uril is able to form a host-guest complex with the neurotransmitter serotonin. In this case, the binding affinity is pH-dependent. The results demonstrate promising biological applications in the delivery and pH-controlled release of serotonin. Saleh et al. described the use of cucurbit[7]uril as a liver protective agent and an adjuvant in toxicological pharmacology. The protective effects of cucurbit[7]uril were evaluated in the biochemical study of the extracted livers of mice following cyanobacterial crude extract treatment with or without cucurbit[7]uril. The addition of cucurbit[7]uril has been shown to significantly reduce the toxicity of cyanotoxin-induced hepatotoxicity (P < 0.05) in vivo. Supramolecular chemistry is useful in the controlled and/or local delivery of immunomodulatory drugs, as reviewed by Soni et al.. In their review, macrocycles such as cyclodextrins are highlighted for Edited and reviewed by: Tony D. James, University of Bath, United Kingdom