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Design, synthesis, and structure-activity relationships of indole-3-heterocycles as agonists of the CB1 receptor.

Abstract：

:Novel indole-3-heterocycles were designed and synthesized and found to be potent CB1 receptor agonists. Starting from a microsomally unstable lead 1, a bioisostere approach replacing a piperazine amide was undertaken. This was found to be a good strategy for improving stability both in vitro and in vivo. This led to the discovery of 24, which had an increased duration of action in the mouse tail flick test in comparison to the lead 1.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Morrison AJ,Adam JM,Baker JA,Campbell RA,Clark JK,Cottney JE,Deehan M,Easson AM,Fields R,Francis S,Jeremiah F,Keddie N,Kiyoi T,McArthur DR,Meyer K,Ratcliffe PD,Schulz J,Wishart G,Yoshiizumi K

doi

10.1016/j.bmcl.2010.10.093

subject

Has Abstract

pub_date

2011-01-01 00:00:00

pages

506-9

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)01554-4

journal_volume

21

pub_type

杂志文章

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