Article

Structure-activity relationships of chiral selective norepinephrine reuptake inhibitors (sNRI) with increased oxidative stability.

Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
Bioorganic & medicinal chemistry letters (impact factor: 2.65). 08/2008; 18(16):4491-4. DOI:10.1016/j.bmcl.2008.07.049 pp.4491-4
Source: PubMed

ABSTRACT The synthesis and SAR of a series of chiral heterocyclic ring-constrained norepinephrine reuptake inhibitors are described. The best compounds compare favorably with atomoxetine in potency (IC(50)s<10 nM), selectivity against the other monoamine transporters, and inhibition of CYP2D6 (IC(50)s>1 microM). In addition, the compounds are generally more stable than atomoxetine to oxidative metabolism and thus are likely to have lower clearance in humans.

0 0
 · 
0 Bookmarks
 · 
53 Views
Data provided are for informational purposes only. Although carefully collected, accuracy cannot be guaranteed. The impact factor represents a rough estimation of the journal's impact factor and does not reflect the actual current impact factor. Publisher conditions are provided by RoMEO. Differing provisions from the publisher's actual policy or licence agreement may be applicable.

Keywords

chiral heterocyclic ring-constrained norepinephrine reuptake inhibitors
 
compounds
 
inhibition
 
lower clearance
 
oxidative metabolism
 
SAR
 
selectivity
 

Sarah Hudson