کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10592873 | 981798 | 2014 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Simplified captopril analogues as NDM-1 inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله

چکیده انگلیسی
Captopril is a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 value of 7.9 μM. It is composed of two units: a 3-mercapto-2-methylpropanoyl fragment and a proline residue. In this study, we synthesized simple amide derivatives of 3-mercapto-2-methylpropanoic acid, and then tested them as NDM-1 inhibitors in order to identify the pharmacophore for NDM-1 inhibition. We found that the lead compound 22 had an IC50 value of 1.0 μM. Further structure simplification provided compounds 31 and 32, which had IC50 values of 15 and 10 μM, respectively. As compound 32 is a clinically used antidote for metal poisoning, it has great potential to be repurposed to treat bacterial infections.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 1, 1 January 2014, Pages 386-389
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 1, 1 January 2014, Pages 386-389
نویسندگان
Ningning Li, Yintong Xu, Qiang Xia, Cuigai Bai, Taiyi Wang, Lei Wang, Dingdi He, Nannan Xie, Lixin Li, Jing Wang, Hong-Gang Zhou, Feng Xu, Cheng Yang, Quan Zhang, Zheng Yin, Yu Guo, Yue Chen,