Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1

Mark Andrews; Alan Brown; Jean-Yves Chiva; David Fradet; David Gordon; Mark Lansdell; Malcolm MacKenny

doi:10.1016/j.bmcl.2009.02.054

Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2329-32. doi: 10.1016/j.bmcl.2009.02.054. Epub 2009 Feb 20.

Authors

Mark Andrews¹, Alan Brown, Jean-Yves Chiva, David Fradet, David Gordon, Mark Lansdell, Malcolm MacKenny

Affiliation

¹ Discovery Chemistry, Pfizer Global Research and Development, Sandwich, United Kingdom.

PMID: 19282174
DOI: 10.1016/j.bmcl.2009.02.054

Abstract

The reported selective serotonin Re-uptake Inhibitor Litoxetine was used as the starting point in the design of a range of potential SSRIs with high ease of synthetic accessibility. Preparation and subsequent optimization yielded a range of potent and highly selective SSRIs.

Publication types

Comparative Study

MeSH terms

Cell Line
Drug Design*
Humans
Piperidines / chemical synthesis
Piperidines / metabolism
Selective Serotonin Reuptake Inhibitors / chemical synthesis*
Selective Serotonin Reuptake Inhibitors / metabolism
Structure-Activity Relationship

Substances

Piperidines
Serotonin Uptake Inhibitors
litoxetine