Synthesis of N-(3-arylprop-2-ynyl)substituted olanzapine derivatives as potential inhibitors of PDE4B

Babu, P. Vijaya, Gorja, Dhilli Rao, Meda, Chandana Lakshmi T., Deora, Girdhar Singh, Kolli, Sunder Kumar, Parsa, Kishore V. L., Mukkanti, K. and Pal, Manojit (2014) Synthesis of N-(3-arylprop-2-ynyl)substituted olanzapine derivatives as potential inhibitors of PDE4B. Tetrahedron Letters, 55 20: 3176-3180. doi:10.1016/j.tetlet.2014.04.009

Attached Files (Some files may be inaccessible until you login with your UQ eSpace credentials)
Name Description MIMEType Size Downloads
UQ331102OA.pdf Full text (open access) application/pdf 746.56KB 0

Author Babu, P. Vijaya
Gorja, Dhilli Rao
Meda, Chandana Lakshmi T.
Deora, Girdhar Singh
Kolli, Sunder Kumar
Parsa, Kishore V. L.
Mukkanti, K.
Pal, Manojit
Title Synthesis of N-(3-arylprop-2-ynyl)substituted olanzapine derivatives as potential inhibitors of PDE4B
Journal name Tetrahedron Letters   Check publisher's open access policy
ISSN 1873-3581
0040-4039
Publication date 2014-05-14
Year available 2014
Sub-type Article (original research)
DOI 10.1016/j.tetlet.2014.04.009
Volume 55
Issue 20
Start page 3176
End page 3180
Total pages 5
Place of publication Kidlington, Oxford United Kingdom
Publisher Pergamon Press
Language eng
Abstract The linkage between dopamine D2 receptors and PDE activity via cAMP prompted us to design a series of novel N-(3-arylprop-2-ynyl)substituted olanzapine derivatives as potential inhibitors of PDE4B. The target compounds were conveniently prepared by using a simple and inexpensive method involving Pd/C-mediated CC bond forming reaction under Sonogashira conditions. A number of compounds were synthesized by using this strategy in good yields. Some of the compounds showed promising inhibition of PDE4B when tested in vitro that was supported by the docking studies.
Keyword Olanzapine
Alkyne
PDE4
Docking
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2015 Collection
School of Pharmacy Publications
 
Versions
Version Filter Type
Citation counts: TR Web of Science Citation Count  Cited 2 times in Thomson Reuters Web of Science Article | Citations
Scopus Citation Count Cited 3 times in Scopus Article | Citations
Google Scholar Search Google Scholar
Created: Tue, 27 May 2014, 10:20:01 EST by System User on behalf of School of Pharmacy