1187189-70-3Relevant academic research and scientific papers
Design and synthesis of boron-containing PDE4 inhibitors using soft-drug strategy for potential dermatologic anti-inflammatory application
Zhang, Yong-Kang,Plattner, Jacob J.,Akama, Tsutomu,Baker, Stephen J.,Hernandez, Vincent S.,Sanders, Virginia,Freund, Yvonne,Kimura, Richard,Bu, Wei,Hold, Karin M.,Lu, Xiao-Song
, p. 2270 - 2274 (2010)
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 IC50 = 47 nM of compound 2) and low emetic activity. These compounds are intended for dermatological use further limiting possible systemic side effects.
Boron-Containing Small Molecules as Anti-Inflammatory Agents
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Paragraph 0916, (2015/11/16)
Compounds and methods of treating anti-inflammatory conditions are disclosed.
