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Design, synthesis, and biological investigation of selective human carbonic anhydrase II, IX, and XII inhibitors using 7-aryl/heteroaryl triazolopyrimidines bearing a sulfanilamide scaffold by Romeo Romagnoli; Tiziano De Ventura; Stefano Manfredini; Erika Baldini; Claudiu T. Supuran; Alessio Nocentini; Andrea Brancale; Roberta Bortolozzi; Lorenzo Manfreda; Giampietro Viola is a Chemistry article available to read on EtoBox.

What is Design, synthesis, and biological investigation of selective human carbonic anhydrase II, IX, and XII inhibitors using 7-aryl/heteroaryl triazolopyrimidines bearing a sulfanilamide scaffold about?

## Abstract A novel library of human carbonic anhydrase (hCA) inhibitors based on the 2-sulfanilamido[1,2,4]triazolo[1,5-__a__]pyrimidine skeleton modified at its 7-position was prepared by an efficient convergent procedure. These derivatives were evaluated __in vitro__ for their inhibition properties against a representative panel of hCA isoforms (hCA I, II, IV, IX, and XII). The target tumour-associated isoforms hCA IX and XII were potently inhibited with __K__~I~s in the low nanomolar range of 5–96 nM and 4–72 nM, respectively. Compounds **1d**, **1j**, **1v**, and **1x** were the most potent hCA IX inhibitors with __K__~I~s of 5.1, 8.6, 4.7, and 5.1 nM, respectively. Along with derivatives **1d** and **1j**, compounds **1r** and **1ab** potently inhibited hCA XII isoform with __K__~I~s in a single-digit nanomolar range of 8.8, 5.4, 4.3, and 9.0 nM, respectively. Compounds **1e**, **1m**, and **1p** exhibited the best selectivity against hCA IX and hCA XII isoforms over off-target hCA II, with selectivity indexes ranging from 5 to 14.

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Author

Romeo Romagnoli; Tiziano De Ventura; Stefano Manfredini; Erika Baldini; Claudiu T. Supuran; Alessio Nocentini; Andrea Brancale; Roberta Bortolozzi; Lorenzo Manfreda; Giampietro Viola

Publisher

Informa UK Limited

Published

2023

Field

Chemistry (Physical Sciences)