Journal
MINI-REVIEWS IN MEDICINAL CHEMISTRY
Volume 11, Issue 12, Pages 1009-1018Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/138955711797247734
Keywords
16-membered macrolides; structural flexibility; mycarose moiety; antimicrobial properties; resistant strains; resistance mechanism; tylosin; leucomycin
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Funding
- National Natural Science Foundation of China [20872081, 21072114]
- Major R&D Program of New Drugs-National S&T Key Special Subject of China [2009ZX09103-115]
- Natural Science Foundation of Shandong [ZR2010HM092]
- SRF for ROCS, SEM
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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.
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