کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10593971 | 981818 | 2011 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis of various 3-nitropropionamides as Mycobacterium tuberculosis isocitrate lyase inhibitor
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis of various 3-nitropropionamides as Mycobacterium tuberculosis isocitrate lyase inhibitor Synthesis of various 3-nitropropionamides as Mycobacterium tuberculosis isocitrate lyase inhibitor](/preview/png/10593971.png)
چکیده انگلیسی
Various 3-nitropropionamides were synthesized and evaluated for in vitro activities against log and starved phase culture of two mycobacterial species and Mycobacterium tuberculosis (MTB) isocitrate lyase (ICL) enzyme inhibition studies. Among 22 compounds, 1-cyclopropyl-7-(3,5-dimethyl-4-(3-nitropropanoyl)piperazin-1-yl)-6-fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (22) was found to be the most active compound in vitro with MICs of 0.16 and 0.04 μM against log- and starved-phase culture of MTB. Compound 22 also showed good enzyme inhibition of MTB ICL with IC50 of 0.10 ± 0.01 μM. The docking studies also confirmed the binding potential of the compounds at the ICL active site.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 18, 15 September 2011, Pages 5149-5154
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 18, 15 September 2011, Pages 5149-5154
نویسندگان
Dharmarajan Sriram, Perumal Yogeeswari, Swetha Methuku, Devambatla Ravi Kumar Vyas, Palaniappan Senthilkumar, Mallika Alvala, Variam Ullas Jeankumar,