Discovery of novel 1,4-dihydropyridine-based PDE4 inhibitors |
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| Authors: | Rajamohan R Poondra Ratnam V Nallamelli Chandana Lakshmi Teja Meda BNV Srinivas Anushka Grover Jyotsna Muttabathula Sreedhara R Voleti Balasubramanian Sridhar Manojit Pal Kishore VL Parsa |
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| Institution: | 1. Department of Medicinal Chemistry, Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500 046, India;2. Department of Biology, Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500 046, India;3. Department of CADD, Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500 046, India;4. Laboratory of X-ray Crystallography, Indian Institute of Chemical Technology, Hyderabad 500 607, India |
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| Abstract: | Substituted 1,4-dihydropyridines were discovered as a novel and potent series of phosphodiesterase 4 (PDE4) inhibitors. Structure–activity relationships within this series have been carried out and studies revealed that the dihydropyridine core, with indole moiety and 3,4-dimethoxybenzyl group, is a potent analogue for PDE4 inhibition. These novel series of compounds were prepared via a 3-component reaction in a single pot. In vitro biological activity, modeling studies and crystallography data are also reported. |
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