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- Title
Assessment of the intraocular pressure-lowering activity of bicyclic derivatives of 1-substituted benzyloctahydroisoquinoline.
- Authors
Saha, Shankar L.; Igbo, Immaculata N.; Opere, Catherine A.; Zhan, Guilin L.; Taniyama, Janis; Ohia, Sunny E.; Roche, Victoria F.; Saha, S L; Igbo, I N; Opere, C A; Zhan, G L; Taniyama, J; Ohia, S E; Roche, V F
- Abstract
In our study of IOP-lowering agents, we have synthesized several bicyclic analogs of 1-benzyloctahydroisoquinoline. The target molecules were synthesized in an eleven-step process. Structures were proved through spectrometry, elemental analysis and, in selected cases, high resolution mass spectrometry. The final products were secondary or tertiary amines containing a 1-benzyl moiety substituted at the p-position with a methoxy, methyl or chloro group. All target molecules were analyzed in 1% solution in distilled water in normotensive rabbits. After topical administration, IOP was monitored in both eyes for up to seven hours. The 1-p-methoxybenzyl molecule 2 was the most active, and caused a maximal IOP drop of 8.8 +/- 1.9 (n = 7) mm Hg in the ipsilateral eye at 4 hours post-administration, with only partial recovery at seven hours. All other compounds tested either showed very weak activity (3-6) or were inactive (1). All compounds produced a contralateral effect, and 5 induced rebound ocular hypertension. We conclude that selected tertiary bicyclic 1-p-methoxybenzyl-octahydroisoquinolines, particularly N-methylated structures, exhibit a significant IOP-lowering effect in normotensive rabbits.
- Subjects
INTRAOCULAR pressure; HIGH resolution spectroscopy; BICYCLIC compounds
- Publication
Journal of Ocular Pharmacology & Therapeutics, 2001, Vol 17, Issue 5, p413
- ISSN
1080-7683
- Publication type
journal article
- DOI
10.1089/108076801753266794