Synthesis and Human Carbonic Anhydrase I, II, IX, and XII Inhibition Studies of Sulphonamides Incorporating Mono-, Bi- and Tricyclic Imide Moieties

New derivatives were synthesised by reaction of amino-containing aromatic sulphonamides with mono-, bi-, and tricyclic anhydrides. These sulphonamides were investigated as human carbonic anhydrases (hCAs, EC 4.2.1.1) I, II, IX, and XII inhibitors. hCA I was inhibited with inhibition constants (Kis)...

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Bibliographic Details
Published in:Pharmaceuticals
Main Authors: Kalyan K. Sethi, KM Abha Mishra, Saurabh M. Verma, Daniela Vullo, Fabrizio Carta, Claudiu T. Supuran
Format: Article
Language:English
Published: MDPI AG 2021-07-01
Subjects:
human carbonic anhydrase inhibitors
benzenesulphonamide
anhydride
docking
SAR
Online Access:https://www.mdpi.com/1424-8247/14/7/693
Description
Summary:New derivatives were synthesised by reaction of amino-containing aromatic sulphonamides with mono-, bi-, and tricyclic anhydrides. These sulphonamides were investigated as human carbonic anhydrases (hCAs, EC 4.2.1.1) I, II, IX, and XII inhibitors. hCA I was inhibited with inhibition constants (Kis) ranging from 49 to >10,000 nM. The physiologically dominant hCA II was significantly inhibited by most of the sulphonamide with the Kis ranging between 2.4 and 4515 nM. hCA IX and hCA XII were inhibited by these sulphonamides in the range of 9.7 to 7766 nM and 14 to 316 nM, respectively. The structure–activity relationships (SAR) are rationalised with the help of molecular docking studies.
ISSN:1424-8247

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