کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1373093 981890 2009 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Pyrazole NNRTIs 4: Selection of UK-453,061 (lersivirine) as a Development Candidate
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Pyrazole NNRTIs 4: Selection of UK-453,061 (lersivirine) as a Development Candidate
چکیده انگلیسی

We prepared three discreet cohorts of potent non-nucleoside HIV reverse transcriptase inhibitors (NNRTIs) based on the recently reported 3-cyanophenoxypyrazole lead 3. Several of these compounds displayed very promising anti-HIV activity in vitro, safety, pharmacokinetic and pharmaceutical profiles. We describe our analysis and conclusions leading to the selection of alcohol 5 (UK-453,061, lersivirine) for clinical development.

We prepared three discreet cohorts of potent non-nucleoside HIV reverse transcriptase inhibitors (NNRTIs) based on the recently reported 3-cyanophenoxypyrazole lead 2. Several of these compounds displayed very promising anti-HIV activity in vitro, safety, pharmacokinetic and pharmaceutical profiles. We describe our analysis and conclusions leading to the selection of alcohol 5 (UK-453,061, lersivirine) for clinical development.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 20, 15 October 2009, Pages 5857–5860
نویسندگان
, , , , , , , , , , , , ,