کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1368832 981729 2014 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Novel indole based NNRTIs with improved potency against wild type and resistant HIV
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Novel indole based NNRTIs with improved potency against wild type and resistant HIV
چکیده انگلیسی

The human immunodeficiency virus (HIV) pandemic remains a significant problem, especially in developing nations where the social and economic impacts are severe. Until a cure or vaccine for the disease is found, a constant supply of new compounds to fill the drug development pipeline is a requirement, given the tendency for the virus to rapidly develop resistance to current therapies. Here we disclose our efforts to improve upon the efficacy of cyclopropyl-indole derivatives developed as NNRTIs in our laboratories. To this end, modifications to the functionality occupying the small Val179 pocket have resulted in nearly two orders of magnitude increase in potency.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 18, 15 September 2014, Pages 4376–4380
نویسندگان
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