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

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

doi:10.1016/j.bmcl.2007.03.073

Novel benzodifuran analogs as potent 5-HT_2A receptor agonists with ocular hypotensive activity

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

Research output: Contribution to journal › Article › peer-review

28 Scopus citations

Abstract

A series of 8-substituted benzodifuran analogs was prepared and evaluated for 5-HT_2A 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 language	English
Pages (from-to)	2998-3002
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	17
Issue number	11
DOIs	https://doi.org/10.1016/j.bmcl.2007.03.073
State	Published - 1 Jun 2007

Keywords

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

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10.1016/j.bmcl.2007.03.073

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title = "Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity",

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%.",

keywords = "(R)-DOI, 5-HT agonist, Benzodifuran, Glaucoma, IOP, Oxadiazole",

author = "Zixia Feng and Suchismita Mohapatra and Klimko, {Peter G.} and Hellberg, {Mark R.} and May, {Jesse A.} and Curtis Kelly and Gary Williams and McLaughlin, {Marsha A.} and Sharif, {Najam A.}",

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T1 - Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity

AU - Feng, Zixia

AU - Mohapatra, Suchismita

AU - Klimko, Peter G.

AU - Hellberg, Mark R.

AU - May, Jesse A.

AU - Kelly, Curtis

AU - Williams, Gary

AU - McLaughlin, Marsha A.

AU - Sharif, Najam A.

PY - 2007/6/1

Y1 - 2007/6/1

N2 - 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%.

AB - 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%.

KW - (R)-DOI

KW - 5-HT agonist

KW - Benzodifuran

KW - Glaucoma

KW - IOP

KW - Oxadiazole

UR - http://www.scopus.com/inward/record.url?scp=34247895609&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2007.03.073

DO - 10.1016/j.bmcl.2007.03.073

M3 - Article

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AN - SCOPUS:34247895609

SN - 0960-894X

VL - 17

SP - 2998

EP - 3002

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 11

ER -

Novel benzodifuran analogs as potent 5-HT_2A receptor agonists with ocular hypotensive activity

Abstract

Keywords

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