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ABSTRACT:
SUBMITTER: D'Ascenzio M
PROVIDER: S-EPMC6009879 | biostudies-literature | 2017 Dec
REPOSITORIES: biostudies-literature
Journal of enzyme inhibition and medicinal chemistry 20161026 1
A large number of novel secondary sulfonamides based on the open saccharin scaffold were synthesized and evaluated as selective inhibitors of four different isoforms of human carbonic anhydrase (hCA I, II, IX and XII, EC 4.2.1.1). They were obtained by reductive ring opening of the newly synthesized N-alkylated saccharin derivatives and were shown to be inactive against the two cytosolic off-target hCA I and II (K<sub>i</sub>s > 10 µM). Interestingly, these compounds inhibited hCA IX in the low ...[more]