Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2

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

doi:10.1016/j.bmcl.2009.08.066

Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2

Bioorg Med Chem Lett. 2009 Oct 15;19(20):5893-7. doi: 10.1016/j.bmcl.2009.08.066. Epub 2009 Aug 21.

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: 19740658
DOI: 10.1016/j.bmcl.2009.08.066

Abstract

A second wave of potential SSRIs with high ease of synthetic accessibility were designed based on the reported selective serotonin re-uptake inhibitor litoxetine and our own previous work in this area. Preparation and subsequent optimisation yielded a range of potent and highly selective SSRIs.

MeSH terms

Adrenergic Uptake Inhibitors / chemistry
Adrenergic Uptake Inhibitors / pharmacology
Antidepressive Agents / chemical synthesis
Antidepressive Agents / chemistry*
Antidepressive Agents / pharmacology
Dopamine Uptake Inhibitors / chemistry
Dopamine Uptake Inhibitors / pharmacology
Drug Design
Selective Serotonin Reuptake Inhibitors / chemical synthesis
Selective Serotonin Reuptake Inhibitors / chemistry*
Selective Serotonin Reuptake Inhibitors / pharmacology
Serotonin Plasma Membrane Transport Proteins / chemistry*
Serotonin Plasma Membrane Transport Proteins / metabolism
Structure-Activity Relationship

Substances

Adrenergic Uptake Inhibitors
Antidepressive Agents
Dopamine Uptake Inhibitors
Serotonin Plasma Membrane Transport Proteins
Serotonin Uptake Inhibitors