Related Experiment Video
Updated: May 13, 2026

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
Novel N-indolylmethyl substituted olanzapine derivatives: their design, synthesis and evaluation as PDE4B inhibitors
Dhilli Rao Gorja1, Soumita Mukherjee, Chandana Lakshmi T Meda
1Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India.
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.
Related Concept Videos
Antipsychotic Drugs: Typical and Atypical Agents
Antidepressant Drugs: MAOIs and Other Agents
Chemotherapy-Induced Nausea and Vomiting: Dopamine Receptor Antagonists
Phenothiazines, such as prochlorperazine...
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
Dipeptidyl Peptidase 4 Inhibitors
Antihypertensive Drugs: Thiazide-Class Diuretics
