1427548-49-9Relevant articles and documents
Novel N-indolylmethyl substituted olanzapine derivatives: Their design, synthesis and evaluation as PDE4B inhibitors
Gorja, Dhilli Rao,Mukherjee, Soumita,Meda, Chandana Lakshmi T.,Deora, Girdhar Singh,Lalith Kumar,Jain, Ankit,Chaudhari, Girish H.,Chennubhotla, Keerthana S.,Banote, Rakesh K.,Kulkarni, Pushkar,Parsa, Kishore V. L.,Mukkanti,Pal, Manojit
supporting information, p. 2075 - 2079 (2013/04/24)
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. The Royal Society of Chemistry 2013.