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
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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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
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 18, 15 September 2014, Pages 4376–4380
نویسندگان
Ronel Müller, Iqbal Mulani, Adriaan E. Basson, Nicole Pribut, Mohammad Hassam, Lynn Morris, Willem A.L. van Otterlo, Stephen C. Pelly,