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Literature DB >> 19303290

Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.

Tsutomu Akama¹, Stephen J Baker, Yong-Kang Zhang, Vincent Hernandez, Huchen Zhou, Virginia Sanders, Yvonne Freund, Richard Kimura, Kirk R Maples, Jacob J Plattner.

Abstract

A series of phenoxy benzoxaboroles were synthesized and screened for their inhibitory activity against PDE4 and cytokine release. 5-(4-Cyanophenoxy)-2,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2728) showed potent activity both in vitro and in vivo. This compound is now in clinical development for the topical treatment of psoriasis and being pursued for the topical treatment of atopic dermatitis.

Entities: Chemical Disease Gene

Mesh：

Substances：

Year: 2009 PMID： 19303290 DOI： 10.1016/j.bmcl.2009.03.007

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

33 in total

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4. A Divalent Protecting Group for Benzoxaboroles.

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5. Discovery of novel benzoxaborole-based potent antitrypanosomal agents.

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Review 10. From the Test Tube to the Treatment Room: Fundamentals of Boron-containing Compounds and their Relevance to Dermatology.

Authors: James Q Del Rosso; Jacob J Plattner
Journal: J Clin Aesthet Dermatol Date: 2014-02

Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.

1. DRM02, a novel phosphodiesterase-4 inhibitor with cutaneous anti-inflammatory activity.

Review 2. Mediators of Chronic Pruritus in Atopic Dermatitis: Getting the Itch Out?

Review 3. Targeting Metalloenzymes for Therapeutic Intervention.

4. A Divalent Protecting Group for Benzoxaboroles.

5. Discovery of novel benzoxaborole-based potent antitrypanosomal agents.

6. Synthesis and evaluation of functionalized benzoboroxoles as potential anti-tuberculosis agents.

7. Ring Structure and Aromatic Substituent Effects on the pK a of the Benzoxaborole Pharmacophore.

8. Characterization of the Dynamic Equilibrium between Closed and Open Forms of the Benzoxaborole Pharmacophore.

9. Natural Product Evodiamine with Borate Trigger Unit: Discovery of Potent Antitumor Agents against Colon Cancer.

Review 10. From the Test Tube to the Treatment Room: Fundamentals of Boron-containing Compounds and their Relevance to Dermatology.