fabrizio carta, Jaydeo T. Kilbile, Suryakant B. Sapkal, Gioele Renzi, Ilaria D’Agostino, Mohamed Boudjelal, Yasinalli Tamboli, Luigi Cutarella, Mattia Mori, Silvia Sgambellone, Serafina Villano, Silvia Marri, Laura Lucarini, Simone Carradori, Claudiu T. Supuran
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引用次数: 0
Abstract
A series of 2,4-dichloro-5-{[4-(phenylsulfonyl)piperazin-1-yl]carbonyl}benzenesulfonamide were designed and synthesized through amidation of Lasamide 1 with substituted piperazines. The newly obtained compounds demonstrated remarkable inhibition potency and selectivity for the human (h) expressed Carbonic Anhydrase (CA; EC 4.2.1.1) II isoform. Selected compounds 7 and 9 were considered in an in vivo model of glaucoma and showed relevant performances with the latter being able to last the effect up to 4 hours. The results herein reported are in sustainment of Lasamide derivatives as a new class of compounds potentially exploitable for the management of uncontrolled IOP.
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