One-Pot Procedure for the Synthesis of Asymmetric Substituted Ureido Benzene Sulfonamides as Effective Inhibitors of Carbonic Anhydrase Enzymes

Autor:	Gioele Vannozzi, Daniela Vullo, Andrea Angeli, Marta Ferraroni, Jacob Combs, Carrie Lomelino, Jacob Andring, Robert Mckenna, Gianluca Bartolucci, Marco Pallecchi, Laura Lucarini, Silvia Sgambellone, Emanuela Masini, Fabrizio Carta, Claudiu T. Supuran
Rok vydání:	2021
Předmět:	Male Models Molecular Sulfonamides Glaucoma Crystallography X-Ray Carbonic Anhydrase II Structure-Activity Relationship Drug Design Drug Discovery Molecular Medicine Animals Rabbits Carbonic Anhydrase Inhibitors Intraocular Pressure Protein Binding
Zdroj:	Journal of medicinal chemistry. 65(1)
ISSN:	1520-4804
Popis:	We report a one-pot procedure for the synthesis of asymmetrical ureido-containing benzenesulfonamides based on in situ generation of the corresponding isocyanatobenezenesulfonamide species, which were trapped with the appropriate amines. A library of new compounds was generated and evaluated in vitro for their inhibition properties against a representative panel of the human (h) metalloenzymes carbonic anhydrases (EC 4.2.1.1), and the best performing compounds on the isozyme II (i.e.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::114fa27d245f828e1b99acd9cb802119 https://pubmed.ncbi.nlm.nih.gov/34958217 Zobrazit plný text záznamu