Synthesis and ocular antihypertensive activity of new imidazolidine derivatives containing a .beta.-blocking side chain
- 1 November 1991
- journal article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 34 (11) , 3197-3204
- https://doi.org/10.1021/jm00115a008
Abstract
The syntheses of new phenylimidazolidine derivatives (3-6)1 containing a propanolamine oxime or an oxypropanolamine moiety attached either to the aromatic or to the imidazolidine ring are described. These compounds were evaluated for potential ocular antihypertensive activity in alpha-chymotrypsin-induced ocular hypertension in rabbits. These compounds represent a unique series of effective ocular antihypertensive agents that despite possessing structural characteristics of beta-blockers and of imidazolidine derivatives, exhibit weak alpha- and beta-adrenergic agonist and antagonist activities. These findings may be of significant therapeutic importance in the medical management of glaucoma.Keywords
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