Gracia, Jordi published the artcileBiphenyl Pyridazinone Derivatives as Inhaled PDE4 Inhibitors: Structural Biology and Structure-Activity Relationships, Name: Methyl 4-fluoro-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate, the publication is Journal of Medicinal Chemistry (2016), 59(23), 10479-10497, database is CAplus and MEDLINE.
Cyclic nucleotide cAMP is an ubiquitous second messenger involved in a plethora of cellular responses to biol. agents involving activation of adenylyl cyclase. Its intracellular levels are tightly controlled by a family of cyclic nucleotide degrading enzymes, the PDEs. In recent years, cyclic nucleotide phosphodiesterase type 4 (PDE4) has aroused scientific attention as a suitable target for anti-inflammatory therapy in respiratory diseases, particularly in the management of asthma and COPD. Here the authors describe efforts to discover novel, highly potent inhaled inhibitors of PDE4. Through structure based design, with the intervention of a wide variety of functional groups and physichochem. profiles to occupy the solvent-filled pocket of the PDE4 enzyme, the authors modified the structure of the authors’ oral PDE4 inhibitors to reach compounds up to picomolar enzymic potencies. In vitro potencies were demonstrated in a rat lung neutrophilia model by suspension microspray administration.
Journal of Medicinal Chemistry published new progress about 757982-31-3. 757982-31-3 belongs to esters-buliding-blocks, auxiliary class Boronic acid and ester,Boronic acid and ester, name is Methyl 4-fluoro-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate, and the molecular formula is C14H18BFO4, Name: Methyl 4-fluoro-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate.
Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics