کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10593995 | 981818 | 2011 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis of rhodamine B-benzenesulfonamide conjugates and their inhibitory activity against human α- and bacterial/fungal β-carbonic anhydrases
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
⺠A series of fluorescent sulfonamide carbonic anhydrase (CA, EC 4.2.1.1) inhibitors were prepared by attaching rhodamine B moieties to the scaffold of benzenesulfonamides. ⺠The compounds have been investigated for the inhibition of 12 human α-CA isoforms (hCA I-hCA XIV), three bacterial and one fungal β-class enzymes from the pathogens Mycobacterium tuberculosis and Candida albicans. ⺠All types of inhibitory activities have been detected, with several compounds showing low nanomolar inhibition against the transmembrane isoforms hCA IX, XII (cancer-associated) and XIV. ⺠The β-CAs were inhibited in the micromolar range by these compounds. ⺠Fluorescent sulfonamide CA inhibitors may have applications for the imaging of hypoxic tumors or of bacteria.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 18, 15 September 2011, Pages 5210-5213
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 18, 15 September 2011, Pages 5210-5213
نویسندگان
Marouan Rami, Alessio Innocenti, Jean-Louis Montero, Andrea Scozzafava, Jean-Yves Winum, Claudiu T. Supuran,