کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1377152 981972 2007 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery of novel non-cytotoxic salicylhydrazide containing HIV-1 integrase inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery of novel non-cytotoxic salicylhydrazide containing HIV-1 integrase inhibitors
چکیده انگلیسی

The previously discovered salicylhydrazide class of compounds displayed potent HIV-1 integrase (IN) inhibitory activity. The development of this class of compounds as antiretroviral agents was halted due to cytotoxicity in the nanomolar to sub-micromolar range. We identified a novel class of non-cytotoxic hydrazide IN inhibitors utilizing the minimally required salicylhydrazide substructure as a template in a small-molecule database search. The novel hydrazides displayed low micromolar IN inhibitory activity and are several hundred-fold less cytotoxic than previously disclosed salicylhydrazide IN inhibitors.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 23, 1 December 2007, Pages 6472–6475
نویسندگان
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