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Issue 13, 2013
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Novel N-indolylmethyl substituted olanzapine derivatives: their design, synthesis and evaluation as PDE4B inhibitors

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Abstract

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.

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

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Publication details

The article was received on 31 Oct 2012, accepted on 11 Feb 2013 and first published on 11 Feb 2013


Article type: Communication
DOI: 10.1039/C3OB27424A
Org. Biomol. Chem., 2013,11, 2075-2079

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

    D. R. Gorja, S. Mukherjee, C. L. T. Meda, G. S. Deora, K. Lalith Kumar, A. Jain, G. H. Chaudhari, K. S. Chennubhotla, R. K. Banote, P. Kulkarni, K. V. L. Parsa, K. Mukkanti and M. Pal, Org. Biomol. Chem., 2013, 11, 2075
    DOI: 10.1039/C3OB27424A

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