Hydrophilic derivatives of an earlier described series of carbonic anhydrase inhibitors have been designed, prepared and profiled against a panel of carbonic anhydrase isoforms, including the glaucoma-related hCA II. For all hydrophilic derivatives, computational prediction of intraocular permeability routes showed the predominance of conjunctival rather than corneal absorption. The potentially reactive primary or secondary amine periphery of these compounds makes them suitable candidates for bioconjugation to polymeric drug carriers. As was shown previously, the most active hCA II inhibitor is efficacious in alleviating intraocular pressure in normotensive rabbits with efficacy matching that of dorzolamide.

5-(Sulfamoyl)thien-2-yl 1,3-oxazole inhibitors of carbonic anhydrase II with hydrophilic periphery / Kalinin, Stanislav; Kovalenko, Alexander; Valtari, Annika; Nocentini, Alessio; Gureev, Maxim; Urtti, Arto; Korsakov, Mikhail; Supuran, Claudiu T; Krasavin, Mikhail. - In: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY. - ISSN 1475-6374. - ELETTRONICO. - 37:(2022), pp. 1005-1011. [10.1080/14756366.2022.2056733]

5-(Sulfamoyl)thien-2-yl 1,3-oxazole inhibitors of carbonic anhydrase II with hydrophilic periphery

Nocentini, Alessio;Supuran, Claudiu T;
2022

Abstract

Hydrophilic derivatives of an earlier described series of carbonic anhydrase inhibitors have been designed, prepared and profiled against a panel of carbonic anhydrase isoforms, including the glaucoma-related hCA II. For all hydrophilic derivatives, computational prediction of intraocular permeability routes showed the predominance of conjunctival rather than corneal absorption. The potentially reactive primary or secondary amine periphery of these compounds makes them suitable candidates for bioconjugation to polymeric drug carriers. As was shown previously, the most active hCA II inhibitor is efficacious in alleviating intraocular pressure in normotensive rabbits with efficacy matching that of dorzolamide.
37
1005
1011
Kalinin, Stanislav; Kovalenko, Alexander; Valtari, Annika; Nocentini, Alessio; Gureev, Maxim; Urtti, Arto; Korsakov, Mikhail; Supuran, Claudiu T; Krasavin, Mikhail
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2158/1289746
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