Novel N-indolylmethyl substituted olanzapine derivatives: their design, synthesis and evaluation as PDE4B inhibitors

Dhilli Rao Gorja; Soumita Mukherjee; Chandana Lakshmi T. Meda; Girdhar Singh Deora; K. Lalith Kumar; Ankit Jain; Girish H. Chaudhari; Keerthana S. Chennubhotla; Rakesh K. Banote; Pushkar Kulkarni; Kishore V. L. Parsa; K. Mukkanti; Manojit Pal

doi:10.1039/C3OB27424A

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Organic & Biomolecular Chemistry

Issue 13, 2013

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Novel N-indolylmethyl substituted olanzapine derivatives: their design, synthesis and evaluation as PDE4B inhibitors

Dhilli Rao Gorja,^a^b Soumita Mukherjee,^a Chandana Lakshmi T. Meda,^a Girdhar Singh Deora,^a K. Lalith Kumar,^a Ankit Jain,^a^c Girish H. Chaudhari,^a^c Keerthana S. Chennubhotla,^a^c Rakesh K. Banote,^a^c Pushkar Kulkarni,^a^c Kishore V. L. Parsa,*^a K. Mukkanti^b and Manojit Pal*^a

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Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India
E-mail: manojitpal@rediffmail.com

Chemistry Division, Institute of Science and Technology, JNT University, Kukatpally, Hyderabad 500072, India

Zephase Therapeutics Pvt. Ltd (An incubated company at the Institute of Life Sciences), University of Hyderabad Campus, Gachibowli, Hyderabad 500 046, India

Org. Biomol. Chem., 2013,11, 2075-2079

DOI: 10.1039/C3OB27424A
Received 31 Oct 2012, Accepted 11 Feb 2013
First published online 11 Feb 2013

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A new strategy for converting antipsychotic drug olanzapine into PDE4 inhibitors is described via the design and Pd/C mediated synthesis of novel N-indolylmethyl olanzapine derivatives. One compound showed good inhibition (IC₅₀ 1.1 μM) and >10 fold selectivity towards PDE4B over D that was supported by docking studies. This compound also showed significant inhibition of TNF-α and no major toxicities in cell lines and a zebrafish embryo model except the teratogenic effects to be re-assessed in rodents.

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Novel N-indolylmethyl substituted olanzapine derivatives: their design, synthesis and evaluation as PDE4B inhibitors

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