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Cu-mediated 1,3-dipolar cycloaddition of azomethine ylides with dipolarophiles: a faster access to spirooxindoles of potential pharmacological interest |
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| Authors: | Shambhu Nath Singh Sridhar Regati Abir Kumar Paul Mohosin Layek Sarva Jayaprakash K Venkateshwara Reddy Girdhar Singh Deora Soumita Mukherjee Manojit Pal |
| Institution: | 1. Custom Pharmaceuticals Services and Dr. Reddy’s Laboratories Ltd, Bollaram Road, Miyapur, Hyderabad 500049, India;2. Department of Chemistry, JNTUH College of Engineering, JNT University, Kukatpally, Hyderabad 500085, India;3. CMR Engineering College Affiliated to JNTU, Medchal Road, Kandlaykoya, Hyderabad 501401, India;4. Biomolecular Pharmaceutical Chemistry Laboratory, School of Pharmacy, The University of Queensland, 20 Cornwall Street, Woolloongabba, Qld 4102, Australia;5. Dr. Reddy’s Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India |
| Abstract: | CuI facilitated three-component reaction of isatin derivatives, l-proline and terminal alkynes containing an amide or ester functional group. The multi-component reaction (MCR) afforded a faster and practical synthesis of spirooxindole derivatives. A range of novel spirooxindoles were synthesized by using this straightforward and one-pot efficient methodology. A representative compound showed significant inhibition of PDE4B enzyme in vitro and good interactions with this protein in silico. |
| Keywords: | MCR CuI Spirooxindole PDE4B |
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