کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1375558 | 981941 | 2009 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode α-carbonic anhydrases
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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![عکس صفحه اول مقاله: A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode α-carbonic anhydrases A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode α-carbonic anhydrases](/preview/png/1375558.png)
چکیده انگلیسی
A sulfonamide derivative of the antihelmintic drug thiabendazole was prepared and investigated for inhibition of the zinc enzyme carbonic anhydrase CA (EC 4.2.1.1). Mammalian isoforms CA I–XIV and the nematode enzyme of Caenorhabditis elegans CAH-4b were included in this study. Thiabendazole-5-sulfonamide was a very effective inhibitor of CAH-4b and CA IX (KIs of 6.4–9.5 nm) and also inhibited effectively isozymes CA I, II, IV–VII, and XII, with KIs in the range of 17.8–73.2 nM. The high resolution X-ray crystal structure of its adduct with isozyme II evidenced the structural elements responsible for this potent inhibitory activity.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 5, 1 March 2009, Pages 1371–1375
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 5, 1 March 2009, Pages 1371–1375
نویسندگان
Letizia Crocetti, Alfonso Maresca, Claudia Temperini, Rebecca A. Hall, Andrea Scozzafava, Fritz A. Mühlschlegel, Claudiu T. Supuran,