کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1361535 981466 2008 18 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design and synthesis of novel leucomycin analogues modified at the C-3 position. Part II: 3-O-(3-Aryl-2-propenyl)leucomycin analogues
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design and synthesis of novel leucomycin analogues modified at the C-3 position. Part II: 3-O-(3-Aryl-2-propenyl)leucomycin analogues
چکیده انگلیسی

The design and synthesis of 16-membered macrolides modified at the C-3 position are described. Starting from fully protected intermediate (5), appropriate modifications including Heck reaction were performed to furnish 3-O-(3-aryl-2-propenyl)leucomycin A7 analogues (9a–9m). These leucomycin A7 derivatives showed improved in vitro antibacterial activities against clinically important pathogens including erythromycin-resistant Streptococcus pneumoniae (ERSP). SAR analysis of derivatives modified at the C-3 and C-3″ positions suggested that single modification at C-3 or C-3″ was effective for in vitro antibacterial activity.

The design and synthesis of 16-membered macrolides modified at the C-3 position are described. 3-O-(3-Aryl-2-propenyl)leucomycin A7 analogues showed improved in vitro antibacterial activities against clinically important pathogens.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 8, 15 April 2008, Pages 4401–4418
نویسندگان
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