N-Benzyl-N-(pyrrolidin-3-yl)carboxamides as a new class of selective dual serotonin/noradrenaline reuptake inhibitors.

Bioorg Med Chem Lett

Department of Genitourinary Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.

Published: August 2008

The structure-activity relationship and the synthesis of novel N-benzyl-N-(pyrrolidin-3-yl)carboxamides as dual serotonin (5-HT) and noradrenaline (NA) monoamine reuptake inhibitors are described. Compounds such as 18 exhibited dual 5-HT and NA reuptake inhibition, good selectivity over dopamine (DA) reuptake inhibition and drug-like physicochemical properties consistent with CNS target space. Compound 18 was selected for further preclinical evaluation.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2008.06.078DOI Listing

Publication Analysis

Top Keywords

reuptake inhibitors
8
reuptake inhibition
8
n-benzyl-n-pyrrolidin-3-ylcarboxamides class
4
class selective
4
selective dual
4
dual serotonin/noradrenaline
4
reuptake
4
serotonin/noradrenaline reuptake
4
inhibitors structure-activity
4
structure-activity relationship
4

Similar Publications

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!