Discovery of novel 1,4-dihydropyridine-based PDE4 inhibitors. 2013

Rajamohan R Poondra, and Ratnam V Nallamelli, and Chandana Lakshmi Teja Meda, and B N V Srinivas, and Anushka Grover, and Jyotsna Muttabathula, and Sreedhara R Voleti, and Balasubramanian Sridhar, and Manojit Pal, and Kishore V L Parsa
Department of Medicinal Chemistry, Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500 046, India. rajamohanreddyp@ilsresearch.org

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.

UI MeSH Term Description Entries
D004095 Dihydropyridines Pyridine moieties which are partially saturated by the addition of two hydrogen atoms in any position.
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D055808 Drug Discovery The process of finding chemicals for potential therapeutic use. Drug Prospecting,Discovery, Drug,Prospecting, Drug
D058988 Phosphodiesterase 4 Inhibitors Compounds that specifically inhibit PHOSPHODIESTERASE 4. PDE-4 Inhibitor,PDE4 Inhibitor,Phosphodiesterase 4 Inhibitor,Phosphodiesterase Type 4 Inhibitor,PDE-4 Inhibitors,PDE4 Inhibitors,Phosphodiesterase Type 4 Inhibitors,4 Inhibitor, Phosphodiesterase,Inhibitor, PDE-4,Inhibitor, PDE4,Inhibitor, Phosphodiesterase 4,Inhibitors, PDE-4,Inhibitors, PDE4,Inhibitors, Phosphodiesterase 4,PDE 4 Inhibitor,PDE 4 Inhibitors
D018360 Crystallography, X-Ray The study of crystal structure using X-RAY DIFFRACTION techniques. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed) X-Ray Crystallography,Crystallography, X Ray,Crystallography, Xray,X Ray Crystallography,Xray Crystallography,Crystallographies, X Ray,X Ray Crystallographies

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