About this Biochemistry, Genetics and Molecular Biology article
Design and synthesis of boron-containing PDE4 inhibitors using soft-drug strategy for potential dermatologic anti-inflammatory application by Yong-Kang Zhang; Jacob J. Plattner; Tsutomu Akama; Stephen J. Baker; Vincent S. Hernandez; Virginia Sanders; Yvonne Freund; Richard Kimura; Wei Bu; Karin M. Hold; Xiao-Song Lu is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
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.
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- Author
- Yong-Kang Zhang; Jacob J. Plattner; Tsutomu Akama; Stephen J. Baker; Vincent S. Hernandez; Virginia Sanders; Yvonne Freund; Richard Kimura; Wei Bu; Karin M. Hold; Xiao-Song Lu
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)
- Published
- 2010
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)