کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1361281 981460 2012 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
A new class of prolylcarboxypeptidase inhibitors, Part 1: Discovery and evaluation
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
A new class of prolylcarboxypeptidase inhibitors, Part 1: Discovery and evaluation
چکیده انگلیسی

A new structural class of potent prolylcarboxypeptidase (PrCP) inhibitors was discovered by high-throughput screening. The series possesses a tractable SAR profile with sub-nanomolar in vitro IC50 values. Compared to prior inhibitors, the new series demonstrated minimal activity shifts in pure plasma and complete ex vivo plasma target engagement in mouse plasma at the 20 h post-dose time point (po). In addition, the in vivo level of CNS and non-CNS drug exposure was measured.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 8, 15 April 2012, Pages 2811–2817
نویسندگان
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