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

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/...

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Published inTetrahedron letters Vol. 55; no. 20; pp. 3176 - 3180
Main Authors Babu, P. Vijaya, Gorja, Dhilli Rao, Meda, Chandana Lakshmi T., Deora, Girdhar Singh, Kolli, Sunder Kumar, Parsa, Kishore V.L., Mukkanti, K., Pal, Manojit
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier Ltd 14.05.2014
Elsevier
Subjects
Alkyne
Bonding
Chemistry
Chemistry, Organic
Derivatives
Docking
Inhibitors
Olanzapine
PDE4
Physical Sciences
Receptors
Science & Technology
Strategy
Synthesis (chemistry)
Tetrahedrons
Docking
Olanzapine
PDE4
Alkyne
PHOSPHODIESTERASE-4 INHIBITORS
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Summary: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.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
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content type line 23
ISSN:0040-4039
1873-3581
DOI:10.1016/j.tetlet.2014.04.009