First evaluation of organotellurium derivatives as carbonic anhydrase I, II, IV, VII and IX inhibitors.

Abstract:

: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.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Angeli A,Tanini D,Capperucci A,Supuran CT

doi

10.1016/j.bioorg.2017.12.010

subject

Has Abstract

pub_date

2018-02-01 00:00:00

pages

268-272

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(17)30726-5

journal_volume

76

pub_type

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