The synthesis and biological evaluation of a range of novel functionalised benzopyrans as potential potassium channel activators

Elizabeth Tyrrell; Kibur Hunie Tesfa; Iain Greenwood; Alistair Mann

doi:10.1016/j.bmcl.2007.11.135

The synthesis and biological evaluation of a range of novel functionalised benzopyrans as potential potassium channel activators

Elizabeth Tyrrell
, Kibur Hunie Tesfa
, Iain Greenwood
, Alistair Mann

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

Abstract

A range of novel benzopyrans have been synthesised and biologically evaluated for K(ATP) channel activity employing cromakalim 1 as a benchmark K(ATP) channel opener. Although the compounds that were evaluated demonstrated a reduced ability to relax phenylephrine stimulated rat thoracic tissue, we provide evidence that benzopyrans 7a-h may be operating via an alternative mechanism than ATP-sensitive K(+) channel activity.

Original language	English
Pages (from-to)	1237-1240
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	3
DOIs	https://doi.org/10.1016/j.bmcl.2007.11.135
Publication status	Published - 1 Feb 2008

Keywords

Chemistry

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10.1016/j.bmcl.2007.11.135

http://dx.doi.org/10.1016/j.bmcl.2007.11.135

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title = "The synthesis and biological evaluation of a range of novel functionalised benzopyrans as potential potassium channel activators",

abstract = "A range of novel benzopyrans have been synthesised and biologically evaluated for K(ATP) channel activity employing cromakalim 1 as a benchmark K(ATP) channel opener. Although the compounds that were evaluated demonstrated a reduced ability to relax phenylephrine stimulated rat thoracic tissue, we provide evidence that benzopyrans 7a-h may be operating via an alternative mechanism than ATP-sensitive K(+) channel activity.",

keywords = "Chemistry",

author = "Elizabeth Tyrrell and Tesfa, \{Kibur Hunie\} and Iain Greenwood and Alistair Mann",

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doi = "10.1016/j.bmcl.2007.11.135",

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AU - Tyrrell, Elizabeth

AU - Tesfa, Kibur Hunie

AU - Greenwood, Iain

AU - Mann, Alistair

PY - 2008/2/1

Y1 - 2008/2/1

N2 - A range of novel benzopyrans have been synthesised and biologically evaluated for K(ATP) channel activity employing cromakalim 1 as a benchmark K(ATP) channel opener. Although the compounds that were evaluated demonstrated a reduced ability to relax phenylephrine stimulated rat thoracic tissue, we provide evidence that benzopyrans 7a-h may be operating via an alternative mechanism than ATP-sensitive K(+) channel activity.

AB - A range of novel benzopyrans have been synthesised and biologically evaluated for K(ATP) channel activity employing cromakalim 1 as a benchmark K(ATP) channel opener. Although the compounds that were evaluated demonstrated a reduced ability to relax phenylephrine stimulated rat thoracic tissue, we provide evidence that benzopyrans 7a-h may be operating via an alternative mechanism than ATP-sensitive K(+) channel activity.

KW - Chemistry

UR - http://www.ncbi.nlm.nih.gov/pubmed/18191566

U2 - 10.1016/j.bmcl.2007.11.135

DO - 10.1016/j.bmcl.2007.11.135

M3 - Article

C2 - 18191566

SN - 0960-894X

VL - 18

SP - 1237

EP - 1240

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 3

ER -

The synthesis and biological evaluation of a range of novel functionalised benzopyrans as potential potassium channel activators

Abstract

Keywords

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