Carbonic Anhydrase Inhibition with Sulfonamides Incorporating Pyrazole- and Pyridazinecarboxamide Moieties Provides Examples of Isoform-Selective Inhibitors

A series of benzenesulfonamides incorporating pyrazole- and pyridazinecarboxamides decorated with several bulky moieties has been obtained by original procedures. The new derivatives were investigated for the inhibition of four physiologically crucial human carbonic anhydrase (hCA, EC 4.2.2.1.1) iso...

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Autores principales:	Andrea Angeli, Victor Kartsev, Anthi Petrou, Mariana Pinteala, Volodymyr Brovarets, Roman Vydzhak, Svitlana Panchishin, Athina Geronikaki, Claudiu T. Supuran
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	carbonic anhydrase inhibitors metalloenzymes pyrazole derivatives Organic chemistry QD241-441
Acceso en línea:	https://doaj.org/article/aa1769f52e1f4f7da32c13f9256e6dee
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spelling	oai:doaj.org-article:aa1769f52e1f4f7da32c13f9256e6dee2021-11-25T18:29:15ZCarbonic Anhydrase Inhibition with Sulfonamides Incorporating Pyrazole- and Pyridazinecarboxamide Moieties Provides Examples of Isoform-Selective Inhibitors10.3390/molecules262270231420-3049https://doaj.org/article/aa1769f52e1f4f7da32c13f9256e6dee2021-11-01T00:00:00Zhttps://www.mdpi.com/1420-3049/26/22/7023https://doaj.org/toc/1420-3049A series of benzenesulfonamides incorporating pyrazole- and pyridazinecarboxamides decorated with several bulky moieties has been obtained by original procedures. The new derivatives were investigated for the inhibition of four physiologically crucial human carbonic anhydrase (hCA, EC 4.2.2.1.1) isoforms, hCA I and II (cytosolic enzymes) as well as hCA IX and XII (transmembrane, tumor-associated isoforms). Examples of isoform-selective inhibitors were obtained for all four enzymes investigated here, and a computational approach was employed for explaining the observed selectivity, which may be useful in drug design approaches for obtaining inhibitors with pharmacological applications useful as antiglaucoma, diuretic, antitumor or anti-cerebral ischemia drugs.Andrea AngeliVictor KartsevAnthi PetrouMariana PintealaVolodymyr BrovaretsRoman VydzhakSvitlana PanchishinAthina GeronikakiClaudiu T. SupuranMDPI AGarticlecarbonic anhydraseinhibitorsmetalloenzymespyrazole derivativesOrganic chemistryQD241-441ENMolecules, Vol 26, Iss 7023, p 7023 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	carbonic anhydrase inhibitors metalloenzymes pyrazole derivatives Organic chemistry QD241-441
spellingShingle	carbonic anhydrase inhibitors metalloenzymes pyrazole derivatives Organic chemistry QD241-441 Andrea Angeli Victor Kartsev Anthi Petrou Mariana Pinteala Volodymyr Brovarets Roman Vydzhak Svitlana Panchishin Athina Geronikaki Claudiu T. Supuran Carbonic Anhydrase Inhibition with Sulfonamides Incorporating Pyrazole- and Pyridazinecarboxamide Moieties Provides Examples of Isoform-Selective Inhibitors
description	A series of benzenesulfonamides incorporating pyrazole- and pyridazinecarboxamides decorated with several bulky moieties has been obtained by original procedures. The new derivatives were investigated for the inhibition of four physiologically crucial human carbonic anhydrase (hCA, EC 4.2.2.1.1) isoforms, hCA I and II (cytosolic enzymes) as well as hCA IX and XII (transmembrane, tumor-associated isoforms). Examples of isoform-selective inhibitors were obtained for all four enzymes investigated here, and a computational approach was employed for explaining the observed selectivity, which may be useful in drug design approaches for obtaining inhibitors with pharmacological applications useful as antiglaucoma, diuretic, antitumor or anti-cerebral ischemia drugs.
format	article
author	Andrea Angeli Victor Kartsev Anthi Petrou Mariana Pinteala Volodymyr Brovarets Roman Vydzhak Svitlana Panchishin Athina Geronikaki Claudiu T. Supuran
author_facet	Andrea Angeli Victor Kartsev Anthi Petrou Mariana Pinteala Volodymyr Brovarets Roman Vydzhak Svitlana Panchishin Athina Geronikaki Claudiu T. Supuran
author_sort	Andrea Angeli
title	Carbonic Anhydrase Inhibition with Sulfonamides Incorporating Pyrazole- and Pyridazinecarboxamide Moieties Provides Examples of Isoform-Selective Inhibitors
title_short	Carbonic Anhydrase Inhibition with Sulfonamides Incorporating Pyrazole- and Pyridazinecarboxamide Moieties Provides Examples of Isoform-Selective Inhibitors
title_full	Carbonic Anhydrase Inhibition with Sulfonamides Incorporating Pyrazole- and Pyridazinecarboxamide Moieties Provides Examples of Isoform-Selective Inhibitors
title_fullStr	Carbonic Anhydrase Inhibition with Sulfonamides Incorporating Pyrazole- and Pyridazinecarboxamide Moieties Provides Examples of Isoform-Selective Inhibitors
title_full_unstemmed	Carbonic Anhydrase Inhibition with Sulfonamides Incorporating Pyrazole- and Pyridazinecarboxamide Moieties Provides Examples of Isoform-Selective Inhibitors
title_sort	carbonic anhydrase inhibition with sulfonamides incorporating pyrazole- and pyridazinecarboxamide moieties provides examples of isoform-selective inhibitors
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/aa1769f52e1f4f7da32c13f9256e6dee
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Carbonic Anhydrase Inhibition with Sulfonamides Incorporating Pyrazole- and Pyridazinecarboxamide Moieties Provides Examples of Isoform-Selective Inhibitors

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