کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1375951 981947 2009 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery of a potent, selective and orally bioavailable 3,9-diazaspiro[5.5]undeca-2-one CCR5 antagonist
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery of a potent, selective and orally bioavailable 3,9-diazaspiro[5.5]undeca-2-one CCR5 antagonist
چکیده انگلیسی

Replacement of the cyclic carbamate in our previously disclosed 1-oxa-3,9-diazaspiro[5.5]undecan-2-one template led to the discovery of two novel series of 3,9-diazaspiro[5.5]undecane and undeca-2-one CCR5 antagonists. The synthesis, SAR, and antiviral activities of these two series are described. One compound (32) was found to have attractive combination of antiviral potency, selectivity, and pharmacokinetic profile. The asymmetric synthesis of 32 was also accomplished and both enantiomers were equally potent.

Two novel series of 3,9-diazaspiro[5.5]undecane and undeca-2-one CCR5 antagonists were discovered. The synthesis, SAR, and antiviral activities of these two series are described. Compound 32 was found to have attractive combination of antiviral potency, selectivity, and pharmacokinetic profile.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 1, 1 January 2009, Pages 209–213
نویسندگان
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