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Gorja, Dhilli Rao; Mukherjee, Soumita; Meda, Chandana Lakshmi T; Deora, Girdhar Singh; Kumar, K Lalith; Jain, Ankit; Chaudhari, Girish H; Chennubhotla, Keerthana S; Banote, Rakesh K; Kulkarni, Pushkar; Parsa, Kishore V L; Mukkanti, K; Pal, Manojit
Organic & biomolecular chemistry, 04/2013, Letnik: 11, Številka: 13Journal Article
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.
