1,2,3-Triazoles derived from olanzapine: their synthesis via an ultrasound assisted CuAAC method and evaluation as inhibitors of PDE4B
The antipsychotic drug olanzapine which does not inhibit PDE4 can be converted into the inhibitor of PDE4B via linking its N -10 position with an appropriately N -substituted 1,2,3-triazole moiety through a methylene linker. All these compounds were conveniently prepared by a CuAAC method under ultr...
Gespeichert in:
Veröffentlicht in: | RSC advances 2015, Vol.5 (115), p.94623-94628 |
---|---|
Hauptverfasser: | , , , , , , |
Format: | Artikel |
Sprache: | eng |
Online-Zugang: | Volltext |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
Zusammenfassung: | The antipsychotic drug olanzapine which does not inhibit PDE4 can be converted into the inhibitor of PDE4B
via
linking its
N
-10 position with an appropriately
N
-substituted 1,2,3-triazole moiety through a methylene linker. All these compounds were conveniently prepared by a CuAAC method under ultrasound irradiation at room temperature and evaluated for their PDE4 inhibitory potential
in vitro
. Three of them were identified as selective inhibitors of PDE4B (IC
50
∼ 5–6 μM) over PDE4D. Overall, the present research reports one of the few examples of an ultrasound assisted CuAAC method used in medicinal chemistry. |
---|---|
ISSN: | 2046-2069 2046-2069 |
DOI: | 10.1039/C5RA20380E |