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

1
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research Guwahati, Assam 781101, India
2
Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi 835215, India
3
Neurofarba Department, Università degli Studi di Firenze, Sezione di Farmaceutica e Nutraceutica, Via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, Italy
*
Authors to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Pharmaceuticals 2021, 14(7), 693; https://0-doi-org.brum.beds.ac.uk/10.3390/ph14070693
Received: 30 June 2021 / Revised: 14 July 2021 / Accepted: 14 July 2021 / Published: 19 July 2021
(This article belongs to the Section Medicinal Chemistry)
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. View Full-Text
Keywords: human carbonic anhydrase inhibitors; benzenesulphonamide; anhydride; docking; SAR human carbonic anhydrase inhibitors; benzenesulphonamide; anhydride; docking; SAR
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MDPI and ACS Style

Sethi, K.K.; Mishra, K.A.; Verma, S.M.; Vullo, D.; Carta, F.; Supuran, C.T. Synthesis and Human Carbonic Anhydrase I, II, IX, and XII Inhibition Studies of Sulphonamides Incorporating Mono-, Bi- and Tricyclic Imide Moieties. Pharmaceuticals 2021, 14, 693. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14070693

AMA Style

Sethi KK, Mishra KA, Verma SM, Vullo D, Carta F, Supuran CT. Synthesis and Human Carbonic Anhydrase I, II, IX, and XII Inhibition Studies of Sulphonamides Incorporating Mono-, Bi- and Tricyclic Imide Moieties. Pharmaceuticals. 2021; 14(7):693. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14070693

Chicago/Turabian Style

Sethi, Kalyan K., KM A. Mishra, Saurabh M. Verma, Daniela Vullo, Fabrizio Carta, and Claudiu T. Supuran 2021. "Synthesis and Human Carbonic Anhydrase I, II, IX, and XII Inhibition Studies of Sulphonamides Incorporating Mono-, Bi- and Tricyclic Imide Moieties" Pharmaceuticals 14, no. 7: 693. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14070693

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