Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity

Zixia Feng, Suchismita Acharya, Peter G. Klimko, Mark R. Hellberg, Jesse A. May, Curtis Kelly, Gary Williams, Marsha A. McLaughlin, Najam A. Sharif

Research output: Contribution to journalArticle

19 Scopus citations

Abstract

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%.

Original languageEnglish
Pages (from-to)2998-3002
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number11
DOIs
StatePublished - 1 Jun 2007

Keywords

  • (R)-DOI
  • 5-HT agonist
  • Benzodifuran
  • Glaucoma
  • IOP
  • Oxadiazole

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    Feng, Z., Acharya, S., Klimko, P. G., Hellberg, M. R., May, J. A., Kelly, C., Williams, G., McLaughlin, M. A., & Sharif, N. A. (2007). Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity. Bioorganic and Medicinal Chemistry Letters, 17(11), 2998-3002. https://doi.org/10.1016/j.bmcl.2007.03.073