Carbonic anhydrases (CA, EC 4.2.1.1) are Zinc metalloenzymes and are present throughout most living organisms. Among the catalytically active isoforms are the cytosolic CA I and II, and tumor-associated CA IX and CA XII. The carbonic anhydrase (CA) inhibitory activities of newly synthesized pyrazoline-linked benzenesulfonamides 18-33 against human CA (hCA) isoforms I, II, IX, and XII were measured and compared with that of acetazolamide (AAZ), a standard inhibitor. Potent inhibitory activity against hCA I was exerted by compounds 18-25, with inhibition constant (KI) values of 87.8-244.1 nM, which were greater than that of AAZ (KI, 250.0 nM). Compounds 19, 21, 22, 29, 30, and 32 were proven to have inhibitory activities against hCA IX with KI values (5.5-37.0 nM) that were more effective than or nearly equal to that of AAZ (KI, 25.0 nM). Compounds 20-22, and 30 exerted potent inhibitory activities (KIs, 7.1-10.1 nM) against hCA XII, in comparison with AAZ (KI, 5.7 nM).

Design, synthesis, and carbonic anhydrase inhibition activity of benzenesulfonamide-linked novel pyrazoline derivatives / Abdel-Aziz, Alaa A-M; El-Azab, Adel S; Bua, Silvia; Nocentini, Alessio; Abu El-Enin, Mohamed A; Alanazi, Mohammed M; AlSaif, Nawaf A; Hefnawy, Mohamed M; Supuran, Claudiu T. - In: BIOORGANIC CHEMISTRY. - ISSN 0045-2068. - ELETTRONICO. - 87:(2019), pp. 425-431. [10.1016/j.bioorg.2019.03.052]

Design, synthesis, and carbonic anhydrase inhibition activity of benzenesulfonamide-linked novel pyrazoline derivatives

Bua, Silvia;Nocentini, Alessio;Supuran, Claudiu T
2019

Abstract

Carbonic anhydrases (CA, EC 4.2.1.1) are Zinc metalloenzymes and are present throughout most living organisms. Among the catalytically active isoforms are the cytosolic CA I and II, and tumor-associated CA IX and CA XII. The carbonic anhydrase (CA) inhibitory activities of newly synthesized pyrazoline-linked benzenesulfonamides 18-33 against human CA (hCA) isoforms I, II, IX, and XII were measured and compared with that of acetazolamide (AAZ), a standard inhibitor. Potent inhibitory activity against hCA I was exerted by compounds 18-25, with inhibition constant (KI) values of 87.8-244.1 nM, which were greater than that of AAZ (KI, 250.0 nM). Compounds 19, 21, 22, 29, 30, and 32 were proven to have inhibitory activities against hCA IX with KI values (5.5-37.0 nM) that were more effective than or nearly equal to that of AAZ (KI, 25.0 nM). Compounds 20-22, and 30 exerted potent inhibitory activities (KIs, 7.1-10.1 nM) against hCA XII, in comparison with AAZ (KI, 5.7 nM).
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425
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Abdel-Aziz, Alaa A-M; El-Azab, Adel S; Bua, Silvia; Nocentini, Alessio; Abu El-Enin, Mohamed A; Alanazi, Mohammed M; AlSaif, Nawaf A; Hefnawy, Mohamed M; Supuran, Claudiu T
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2158/1289771
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