کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1370626 | 981823 | 2011 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery and synthesis of a new class of opioid ligand having a 3-azabicyclo[3.1.0]hexane core. An example of a ‘magic methyl’ giving a 35-fold improvement in binding
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
In looking for a novel achiral μ opioid receptor antagonist for the treatment of pruritus, we designed and synthesised azabicyclo[3.1.0]hexane compounds as a new class of opioid ligand. During optimisation, an addition of a single methyl resulted in a 35-fold improvement in binding. An early example from the series had excellent μ opioid receptor antagonist antagonist activity and was very effective in an in vivo pruritus study.
The synthesis and biological evaluation of 3-azabicyclo[3.1.0]hexane mu opioid receptor antagonists 2 and 3 are reported. The significant potency enhancement made by a single methyl substituent is discussed.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 15, 1 August 2011, Pages 4608–4611
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 15, 1 August 2011, Pages 4608–4611
نویسندگان
Graham Lunn, Bernard J. Banks, Robert Crook, Neil Feeder, Alan Pettman, Yogesh Sabnis,