Synthesis and physicochemical properties of sulfamate derivatives as topical antiglaucoma agents.

Autor: Lo YS; A.H. Robins Company, Richmond, Virginia 23261-6609., Nolan JC, Maren TH, Welstead WJ Jr, Gripshover DF, Shamblee DA
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 1992 Dec 25; Vol. 35 (26), pp. 4790-4.
DOI: 10.1021/jm00104a003
Abstrakt: 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.
Databáze: MEDLINE