79617-15-5Relevant academic research and scientific papers
Synthetic method of isotope-labeled erythromycylamine
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, (2020/07/28)
The invention discloses a synthetic method of isotope-labeled erythromycylamine, belongs to the field of drug metabolism, and provides a synthetic method which is reasonable in process design, strongin operability and high in yield, can efficiently convert isotope-labeled raw materials into labeled target products, and can realize industrial production of isotope-labeled erythromycylamine. The method takes 13CD3 labeled methyl iodide as a starting raw material, the isotope-labeled erythromycylamine is synthesized by six steps of reactions, optimal preparation steps and reaction conditions arescreened out through a large number of experiments, the whole process is reasonable in design and high in operability, the labeled raw materials can be efficiently converted into labeled target products, the chemical purity of the labeled erythromycylamine prepared through the method can reach 98.5% or above, and the labeled isotope abundance is larger than 98.5%.
Synthesis and structure-activity relationship of a novel class of 15-membered macrolide antibiotics known as '11a-azalides'
Sugimoto, Tomohiro,Tanikawa, Tetsuya,Suzuki, Keiko,Yamasaki, Yukiko
, p. 5787 - 5801 (2012/11/06)
Macrolide antibiotics are widely prescribed for the treatment of respiratory tract infections; however, the increasing prevalence of macrolide-resistant pathogens is a public health concern. Therefore, the development of new macrolide scaffolds with activities against resistant pathogens is urgently needed. An efficient method for reconstructing the erythromycin A macrolactone skeleton has been established. Based on this methodology, novel 15-membered macrolides, known as '11a-azalides', with substituents at the C12, C13, or C4″ positions were synthesized and their antibacterial activities were evaluated. These derivatives showed promising antibacterial activities against erythromycin-resistant Streptococcus pneumoniae. Among them, the C4″ substituted derivatives had the most potent activity against erythromycin-resistant S. pneumoniae.
Design, synthesis, and biological evaluation of BODIPY-erythromycin probes for bacterial ribosomes
Li, Jing,Kim, In Ho,Roche, Eric D.,Beeman, Doug,Lynch, A. Simon,Ding, Charles Z.,Ma, Zhenkun
, p. 794 - 797 (2007/10/03)
BODIPY-erythromycin probes of bacterial ribosomes were designed and synthesized by attaching a BODIPY fluorophore to the 4″- and 9-positions of the erythromycin structure. The probes exhibited excellent binding affinity to bacterial
