کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1366535 | 981595 | 2007 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A series of 8-substituted benzodifuran analogs was prepared and evaluated for 5-HT2A receptor binding and activation. Several compounds containing ether and ester functionality were found to be potent agonists. Topical ocular administration of 5, 18, and 25 effectively reduced intra-ocular pressure in the hypertensive cynomolgus monkey eye in the range of 25–37%.
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 300 μg doses.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 11, 1 June 2007, Pages 2998–3002
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 11, 1 June 2007, Pages 2998–3002
نویسندگان
Zixia Feng, Suchismita Mohapatra, Peter G. Klimko, Mark R. Hellberg, Jesse A. May, Curtis Kelly, Gary Williams, Marsha A. McLaughlin, Najam A. Sharif,