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  • Title: Synthesis and physicochemical properties of sulfamate derivatives as topical antiglaucoma agents.
    Author: Lo YS, Nolan JC, Maren TH, Welstead WJ, Gripshover DF, Shamblee DA.
    Journal: J Med Chem; 1992 Dec 25; 35(26):4790-4. PubMed ID: 1479580.
    Abstract:
    Several imidazolylphenyl sulfamate and (imidazolylphenoxy)alkyl sulfamate derivatives were synthesized and evaluated as topically active carbonic anhydrase inhibitors. Water solubility, pKa, carbonic anhydrase inhibition, and partition coefficient for the compounds were measured. Sulfamic acid 2-[4-(1H-imidazol-1-yl)phenoxy]ethyl ester monohydrochloride (16) has the best combination of properties and showed excellent topical activity in lowering the intraocular pressure in New Zealand white rabbits.
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