کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1372577 981871 2011 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery of a highly potent series of TLR7 agonists
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery of a highly potent series of TLR7 agonists
چکیده انگلیسی

The discovery of a series of highly potent and novel TLR7 agonist interferon inducers is described. Structure–activity relationships are presented, along with pharmacokinetic studies of a lead molecule from this series of N9-pyridylmethyl-8-oxo-3-deazapurine analogues. A rationale for the very high potency observed is offered. An investigation of the clearance mechanism of this class of compounds in rat was carried out, resulting in aldehyde oxidase mediated oxidation being identified as a key component of the high clearance observed. A possible solution to this problem is discussed.

The discovery of a series of highly potent and novel TLR7 agonist interferon inducers is described. Structure–activity relationships are presented, along with pharmacokinetic studies of a lead molecule from this series of N9-pyridylmethyl-8-oxo-3-deazapurine analogues. An investigation of the clearance mechanism of this class of compounds in rat was carried out, resulting in aldehyde oxidase mediated oxidation being identified as a key component of the high clearance observed.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 19, 1 October 2011, Pages 5939–5943
نویسندگان
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