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Heterocyclic periphery in the design of carbonic anhydrase inhibitors: 1,2,4-Oxadiazol-5-yl benzenesulfonamides as potent and selective inhibitors of cytosolic hCA II and membrane-bound hCA IX isoforms.

Abstract：

:A series of novel aromatic primary sulfonamides decorated with diversely substituted 1,2,4-oxadiazole periphery groups has been prepared using a parallel chemistry approach. The compounds displayed a potent inhibition of cytosolic hCA II and membrane-bound hCA IX isoforms. Due to a different cellular localization of the two target enzymes, the compounds can be viewed as selective inhibition tools for either isoform, depending on the cellular permeability profile. The SAR findings revealed in this study has been well rationalized by docking simulation of the key compounds against the crystal structures of the relevant hCA isoforms.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Krasavin M,Shetnev A,Sharonova T,Baykov S,Tuccinardi T,Kalinin S,Angeli A,Supuran CT

doi

10.1016/j.bioorg.2017.10.005

subject

Has Abstract

pub_date

2018-02-01 00:00:00

pages

88-97

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(17)30682-X

journal_volume

76

pub_type

杂志文章

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