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Published on: October 25, 2024
Recent advances in the field of 16-membered macrolide antibiotics
1Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, P.R. China.
Abstract:
The continuing emergence of bacterial resistance has provided an incentive for recent intensified research on macrolide antibiotics. Belonging to the macrolide family, 16-membered macrolides also experience a renewed interest in further exploration. The medicinal potential of 16-membered macrolides in search for new antibacterials stems from some advantages over 14-membered macrolides, such as gastrointestinal tolerability, structural flexibility, and lack of inducible resistance. Thus, compared with abundant articles on various 14-membered macrolide derivatives in the literature, this review will highlight some representative 16-membered macrolide antibiotics and their recently discovered analogs. Furthermore, the action and resistance mechanisms of 16-membered macrolide antibiotics will be elucidated as well to assist the drug design.
Insights
This review highlights 16-membered macrolide antibiotics, focusing on their potential as new antibacterials. It explores their advantages, mechanisms of action, and resistance to aid in novel drug design.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Microbiology
Background:
- Rising bacterial resistance necessitates novel antibacterial agents.
- Macrolide antibiotics are a key class, with renewed interest in 16-membered variants.
- 16-membered macrolides offer potential advantages over 14-membered counterparts.
Purpose of the Study:
- To review representative 16-membered macrolide antibiotics and their analogs.
- To elucidate the mechanisms of action and resistance for these compounds.
- To provide insights for future antibacterial drug design.
Main Methods:
- Literature review of recent research on 16-membered macrolide antibiotics.
- Analysis of structural features, medicinal potential, and pharmacological properties.
- Examination of bacterial resistance mechanisms and drug action.
Main Results:
- 16-membered macrolides exhibit favorable properties like improved gastrointestinal tolerability and structural flexibility.
- They present a reduced risk of inducible resistance compared to some other macrolides.
- Recent analogs show promise for development as novel antibacterial drugs.
Conclusions:
- 16-membered macrolides represent a promising scaffold for developing new antibacterial therapies.
- Understanding their action and resistance mechanisms is crucial for optimizing drug design.
- Further exploration of these compounds is warranted to combat bacterial resistance.
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