Design and synthesis of boron-containing PDE4 inhibitors using soft-drug strategy for potential dermatologic anti-inflammatory application.
Basic Information
ID: ALA1156280
Journal: Bioorg Med Chem Lett
Title: Design and synthesis of boron-containing PDE4 inhibitors using soft-drug strategy for potential dermatologic anti-inflammatory application.
Authors: Zhang YK, Plattner JJ, Akama T, Baker SJ, Hernandez VS, Sanders V, Freund Y, Kimura R, Bu W, Hold KM, Lu XS.
Abstract: PDE4 inhibitors are a validated approach as anti-inflammatory agents but are limited by systemic side effects including emesis. We report a soft-drug strategy incorporating a carboxylic ester group into boron-containing PDE4 inhibitors leading to the discovery of a series of benzoxaborole compounds with good potency (for example IC(50)=47 nM of compound 2) and low emetic activity. These compounds are intended for dermatological use further limiting possible systemic side effects.
CiteXplore: 20188549
DOI: 10.1016/j.bmcl.2010.02.010
Patent ID: ┄