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Design, synthesis, and structure-activity relationships of indole-3-heterocycles as agonists of the CB1 receptor.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Jan 01; Vol. 21 (1), pp. 506-9. Date of Electronic Publication: 2010 Oct 25. - Publication Year :
- 2011
-
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.<br /> (Copyright © 2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Drug Design
Heterocyclic Compounds chemical synthesis
Heterocyclic Compounds pharmacokinetics
Indoles chemical synthesis
Indoles pharmacokinetics
Mice
Microsomes metabolism
Models, Molecular
Receptor, Cannabinoid, CB1 metabolism
Structure-Activity Relationship
Thiadiazoles chemical synthesis
Thiadiazoles pharmacokinetics
Heterocyclic Compounds chemistry
Indoles chemistry
Receptor, Cannabinoid, CB1 agonists
Thiadiazoles chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21075630
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.10.093