کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1370453 981819 2011 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and preliminary biological evaluation of novel N-(3-aryl-1,2,4-triazol-5-yl) cinnamamide derivatives as potential antimycobacterial agents: An operational Topliss Tree approach
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and preliminary biological evaluation of novel N-(3-aryl-1,2,4-triazol-5-yl) cinnamamide derivatives as potential antimycobacterial agents: An operational Topliss Tree approach
چکیده انگلیسی

A series of novel N-(3-aryl-1,2,4-triazol-5-yl) cinnamamide derivatives were designed on basis of structural similarity to the known FAS II inhibitors. Topliss operational method was used to optimize the potency of molecules. The minimum inhibitory concentration (MIC) of all synthesized compounds was determined against Mycobacterium tuberculosis H37Rv using resazurin microtitre assay (REMA) plate method. The synthesized compounds exhibit antimycobacterial activity in the range of 5–95 μM with a good safety profile.

A novel series of N-(3-aryl-1,2,4-triazol-5-yl) cinnamamide derivatives were synthesized as potential antimycobacterial agents. Topliss operational method was used successfully to optimize the molecules with regards to activity and significant improvement was observed from >90 μM to <5 μM against Mycobacterium tuberculosis H37Rv.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 21, 1 November 2011, Pages 6523–6526
نویسندگان
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