期刊
BIOORGANIC CHEMISTRY
卷 76, 期 -, 页码 88-97出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2017.10.005
关键词
Carbonic anhydrase; Isoform-selective inhibitors; Periphery groups; Primary sulfonamides; Nanomolar inhibition; 1,2,4-Oxadiazole; Acylation; Cyclodehydration; Superbase
资金
- Russian Scientific Fund [14-50-00069]
- Russian Federation Ministry of Education and Science [02.a03.21.0008]
- Russian Science Foundation [14-50-00069] Funding Source: Russian Science Foundation
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. (C) 2017 Published by Elsevier Inc.
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