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

14 5 2014

Authors: P Vijaya Babu, Dhilli Rao Gorja, Chandana Lakshmi T Meda, Girdhar Singh Deora, Sunder Kumar Kolli, Kishore VL Parsa, K Mukkanti, Manojit Pal

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 Csingle bondC 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.