1,2,3-Triazoles derived from olanzapine: their synthesis via an ultrasound assisted CuAAC method and evaluation as inhibitors of PDE4B

The antipsychotic drug olanzapinewhich does not inhibit PDE4 can be converted into the inhibitor of PDE4B via linking its N-10 position with an appropriately N-substituted 1,2,3-triazole moiety through a methylene linker. All these compounds were conveniently prepared by a CuAAC method under ultrasound irradiation at room temperature and evaluated for their PDE4 inhibitory potential in vitro. Three of them were identified as selective inhibitors of PDE4B (IC50 similar to 5-6 mu M) over PDE4D. Overall, the present research reports one of the few examples of an ultrasound assisted CuAAC method used inmedicinal chemistry.