Novel N-indolylmethyl substituted olanzapine derivatives: their design, synthesis and evaluation as PDE4B inhibitorsElectronic supplementary information (ESI) available: 1H and 13C NMR, MS and HRMS data of all new compounds. See DOI: 10.1039/c3ob27424a

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 (IC 50 1.1 μM) and >10 fold selectivity towards PDE4B over D that was supp...

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Main Authors Gorja, Dhilli Rao, Mukherjee, Soumita, Meda, Chandana Lakshmi T, Deora, Girdhar Singh, Lalith Kumar, K, Jain, Ankit, Chaudhari, Girish H, Chennubhotla, Keerthana S, Banote, Rakesh K, Kulkarni, Pushkar, Parsa, Kishore V. L, Mukkanti, K, Pal, Manojit
Format Journal Article
LanguageEnglish
Published 06.03.2013
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Summary: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 (IC 50 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. A new strategy for converting antipsychotic drug olanzapine into PDE4 inhibitors is described.
Bibliography:1
C NMR, MS and HRMS data of all new compounds. See DOI
13
Electronic supplementary information (ESI) available
H and
10.1039/c3ob27424a
ISSN:1477-0520
1477-0539
DOI:10.1039/c3ob27424a