1427548-48-8Relevant 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
, p. 2075 - 2079 (2013)
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.