Affiliation:
1. Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan 250012, China
Abstract
The chemical modification of natural products has been a major method in the discovery
and synthesis of new macrolide antibiotics (MA) to treat a variety of infectious diseases. However, a
lot of MA obtained in the above methods are no longer effective, because the bacteria quickly develop
their resistance to these new macrolides, which has become a great threat to successful treatment of infectious
diseases, such as infections of the respiratory system and urinary system. In this paper, total
synthetic methods for MA that include erythromycin A (ERY), azithromycin (AZM), the clinical candidate
solithromycin (CEM-101), as well as 14-membered and 15-membered azaketolides have been
systematically reviewed on the basis of the literature reported previously. The total synthetic methods
we describe here helps to accelerate the discovery of newer MA to deal with the serious problem of
bacterial resistance.
Funder
National Natural Science Foundation of China
Key Research and Development Project of Shandong Province
Publisher
Bentham Science Publishers Ltd.
Subject
Drug Discovery,Pharmacology,General Medicine
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