Kalinin, Stanislav published the artcileHighly hydrophilic 1,3-oxazol-5-yl benzenesulfonamide inhibitors of carbonic anhydrase II for reduction of glaucoma-related intraocular pressure, Formula: C10H20N2O2, the main research area is glaucoma intraocular pressure CA inhibitors hydrophilicity non corneal absorption; Carbonic anhydrase inhibitors; Glaucoma; Hydrophilicity; Intraocular delivery; Intraocular pressure; Non-corneal absorption.
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 clin. used 2% dorzolamide (Trusopt) eye drops. This indicated that the absorption of the compounds may occur via alternative route across conjunctiva and sclera.
Bioorganic & Medicinal Chemistry published new progress about Carbonic anhydrase inhibitors. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Formula: C10H20N2O2.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem