Репозиторий Университета

Год публикации: Все года 2018 2019 2020

Название	Дата публикации	Коллектив авторов	Журнал	DOI	Индекс цитирования	Ссылка на источник
Highly hydrophilic 1,3-oxazol-5-yl benzenesulfonamide inhibitors of carbonic anhydrase II for reduction of glaucoma-related intraocular pressure Carbonicanhydraseinhibitors Glaucoma Hydrophilicity Intraoculardelivery Intraocularpressure Non-cornealabsorption	01.11.2019	Kalinin S. Valtari A. Ruponen M. Toropainen E. Kovalenko A. Nocentini A. Gureev M. Dar'in D. Urtti A. Supuran C. Krasavin M.	Bioorganic and Medicinal Chemistry	10.1016/j.bmc.2019.115086	0	Ссылка © 2019 Elsevier Ltd Four inhibitors of human carbonic anhydrase II (hCA II) were designed based on the previously reported subnanomolar 1,3-oxazole-based sulfonamide inhibitors of the enzyme to incorporate primary and secondary amine functionality in the carboxamide side chain. The new hydrophilic compounds were found to inhibit the target isoform in sub-nanomolar to low nanomolar range with a good degree of selectivity to several other hCA isoforms. The hydrophilic character of these compounds is advantageous for intraocular residence time but not for corneal permeability which generally requires that a drug be sufficiently lipophilic. Two of the four compounds investigated, however, were found to exert comparable efficacy as 1% eye drops in PBS to that of the clinically used 2% dorzolamide (Trusopt®) eye drops. This indicated that the absorption of the compounds may occur via alternative route across conjunctiva and sclera. Читать тезис

Репозиторий Университета

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