کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1358874 981370 2011 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis and inhibition activity of a novel cyclic enediyne amino acid conjugates against MPtpA
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design, synthesis and inhibition activity of a novel cyclic enediyne amino acid conjugates against MPtpA
چکیده انگلیسی

In course of studies towards the discovery of selective inhibitors of MPtpA, a novel cyclic endiyne malonamic acid has been designed and synthesized. The synthesis involves a crucial intramolecular Knoevenagel reaction. The compound displayed a reversible non-competitive inhibition against MPtpA with inhibition constant Ki of 22.5 μM. The enediyne acts as a recognition framework in inducing the inhibition and not as a reactive functional moiety. This was confirmed by comparing the inhibiting activity with that of the corresponding saturated cyclic non-enediyne analogue.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 10, 15 May 2011, Pages 3274–3279
نویسندگان
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