کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1356296 | 981105 | 2010 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
9-Dihydroerythromycin ethers as motilin agonists—Developing structure–activity relationships for potency and safety
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: 9-Dihydroerythromycin ethers as motilin agonists—Developing structure–activity relationships for potency and safety 9-Dihydroerythromycin ethers as motilin agonists—Developing structure–activity relationships for potency and safety](/preview/png/1356296.png)
چکیده انگلیسی
A series of derivatives of the amine of 9-dihydro-9-O-ethylamino-N-desmethyl-N-isopropyl erythromycin A derivatives were synthesized as motilin agonists. The compounds were developed for potency without showing antibacterial activity and inhibition of the hERG potassium channel. The formamide of the amide series was found to show the optimal combination of properties relative to carbamates, ureas, thioureas, and amines. This prompted an investigation of heterocyclic isosteres for the amide. In this series the triazole had the optimal combination of properties. From the study, two compounds met the criteria for detailed pharmacokinetic studies.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 18, Issue 21, 1 November 2010, Pages 7651–7658
Journal: Bioorganic & Medicinal Chemistry - Volume 18, Issue 21, 1 November 2010, Pages 7651–7658
نویسندگان
Yaoquan Liu, Yong Li, David C. Myles, Mark Claypool, Christopher W. Carreras, Simon J. Shaw,