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Pd-mediated functionalization of polysubstituted pyrroles: Their evaluation as potential inhibitors of PDE4 |
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| Authors: | T Bhaskar Kumar Ch Sumanth S Vaishaly M Srinivasa Rao K B Chandra Sekhar Chandana Lakshmi T Meda Ajit Kandale D Rambabu G Rama Krishna C Malla Reddy K Shiva Kumar Kishore V L Parsa Manojit Pal |
| Affiliation: | Custom Pharmaceutical Services, Dr. Reddy's Laboratories Limited, Bollaram Road Miyapur, Hyderabad 500049, India; Department of Chemistry, Institute of Science and Technology, JNT University of Anantapur, Anantapur 515002, India. |
| Abstract: | Novel polysubstituted pyrroles have been designed and accessed via a one-pot multicomponent reaction followed by Pd-mediated C-C bond forming reactions. All the compounds synthesized were tested for their PDE4B inhibitory properties in vitro and two of them obtained via Heck reaction showed significant inhibition. The docking results suggested that these alkenyl derivatives containing ester moiety interact well with the PDE4B protein in silico where the ester carbonyl oxygen played a key role. The pyrrole framework presented here could be a new template for the identification of small molecule based novel inhibitors of PDE4. The single crystal X-ray data of a representative compound is presented. |
| Keywords: | Pyrrole MCR Palladium Coupling PDE4 |
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