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First evaluation of organotellurium derivatives as carbonic anhydrase I, II, IV, VII and IX inhibitors
Bioorganic Chemistry ( IF 5.1 ) Pub Date : 2017-12-05 , DOI: 10.1016/j.bioorg.2017.12.010
Andrea Angeli , Damiano Tanini , Antonella Capperucci , Claudiu T. Supuran

A series of tellurides was evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors against the human (h) carbonic anhydrase isoforms hCA I, II, IV, VII and IX, involved in a variety of diseases, including glaucoma, retinitis pigmentosa, epilepsy, arthritis and tumors. These compounds, which are the first tellurium-containing derivatives acting as inhibitors of carbonic anhydrase enzymes, showed effective inhibition against all isoforms investigated and some of them were selective for inhibiting the cytosolic or the membrane-bound CAs. Thus, these carbonic anhydrase inhibitors are interesting leads for the development of isoform-selective inhibitors.



中文翻译:

首次评估有机碲衍生物作为碳酸酐酶I,II,IV,VII和IX抑制剂

评估了一系列碲化物作为抗人(h)碳酸酐酶同工型hCA I,II,IV,VII和IX的碳酸酐酶(CA,EC 4.2.1.1)抑制剂,涉及多种疾病,包括青光眼,色素性视网膜炎,癫痫病,关节炎和肿瘤。这些化合物是最早的充当碳酸酐酶抑制剂的含碲衍生物,对所研究的所有同工型均显示出有效的抑制作用,其中某些对抑制胞质或膜结合CA具有选择性。因此,这些碳酸酐酶抑制剂是开发同工型选择性抑制剂的有趣线索。

更新日期:2017-12-05
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