首页> 美国卫生研究院文献>Journal of Enzyme Inhibition and Medicinal Chemistry >New sulfonamides containing organometallic-acylhydrazones: synthesis characterisation and biological evaluation as inhibitors of human carbonic anhydrases
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New sulfonamides containing organometallic-acylhydrazones: synthesis characterisation and biological evaluation as inhibitors of human carbonic anhydrases

机译:含有有机金属酰基hydr的新型磺酰胺类化合物:合成表征和生物学评估可作为人碳酸酐酶的抑制剂

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摘要

A series of organometallic acylhydrazones was prepared, incorporating Re(CO)3, Mn(CO)3 and ferrocenyl moieties, which were subsequently reacted with amino-sulfonamides in order to obtain carbonic anhydrase (CA, EC 4.2.1.1) inhibitors possessing organometallic moieties in their molecules. The new derivatives were investigated as inhibitors of four human (h) CA isoforms with pharmaceutical applications, such as the cytosolic hCA I, II and VII and the mitochondrial hCA VA. An interesting inhibitory profile against these isoforms was obtained, with some of these metal complexes acting as subnanomolar or low nanomolar inhibitors. They were also thoroughly characterised from the chemical point of view, making them of interest for further developments in the field of metal complexes of sulfonamides with CA inhibitory action.
机译:制备了一系列有机金属酰基hydr,其中掺入了Re(CO)3,Mn(CO)3和二茂铁基部分,随后与氨基磺酰胺反应以获得具有有机金属部分的碳酸酐酶(CA,EC 4.2.1.1)抑制剂在他们的分子中。研究了这些新衍生物作为四种人(h)CA同工型的抑制剂,并具有药学应用,例如胞质hCA I,II和VII和线粒体hCA VA。获得了对这些同工型的有趣的抑制特性,其中一些金属络合物充当亚纳摩尔或低纳摩尔抑制剂。还从化学角度对它们进行了彻底的表征,使其成为具有CA抑制作用的磺酰胺金属配合物领域的进一步发展的兴趣。

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