Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity.
Bioorganic & Medicinal Chemistry Letters(2007)
Abstract
A series of benzodifuran analogs with reduced lipophilicity were designed and synthesized as novel 5-HT2A agonists. The selected compounds 5, 18, and 25 exhibited potent and efficacious ocular hypotensive activity in cynomolgus monkey eye, affording maximum IOP reductions of 37%, 27%, and 24%, respectively, at 300μg doses.
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Key words
5-HT2 agonist,Glaucoma,IOP,Benzodifuran,(R)-DOI,Oxadiazole
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