AN2898
(5-(3,4-dicyanophenoxy)-1-hydroxy -1,3-dihydro-2,1-benzoxaborole)
1,2-Benzenedicarbonitrile, 4-((1,3-dihydro-1-hydroxy-2,1-benzoxaborol-5-yl)oxy)-,
AN-2898
cas: 906673-33-4
UNII: 6O60L94RMB,
MW 276.0581, MF C15 H9 B N2 O3
A PDE4 inhibitor potentially for the treatment of fungal infection.
AN-2898, a novel topical anti-inflammatory compound that inhibits phosphodiesterase 4 and 7 enzyme activit
PHASE 2 FUNGAL INFECTION, Anacor Pharmaceuticals for the treatment of atopic dermatitis
| Anacor Pharmaceuticals Inc. | |
| Description | Boron-containing small molecule phosphodiesterase-4 (PDE-4) inhibitor that reduces the production of tumor necrosis factor (TNF) alpha, IL-12 and IL-23 |
| Molecular Target | Phosphodiesterase-4 (PDE-4) |
| Mechanism of Action | Phosphodiesterase-4 (PDE-4) inhibitor |
| Therapeutic Modality | Small molecule |
AN2898 (5-(3,4-dicyanophenoxy)-1-hydroxy -1,3-dihydro-2,1-benzoxaborole) is a broad spectrum anti-inflammatory compound currently in development for the topical treatment of plaque and atopic psoriasis.
AN2898 inhibited phosphodiesterase 4 (PDE4) enzyme activity (IC50 0.060 μM) and the release of multiple cytokines including TNF-α (IC50 0.16 μM) from peripheral blood mononuclear cells (hPBMCs) stimulated by lipopolysaccharide (LPS) or phytohemag- glutinin.
Further, AN2898 was also found to inhibit IL-23 release (IC50 1.0 μM) from THP-1 cells stimulated by LPS and IFN-γ. Investigation of the structure-activity relation-ship around this compound was reported to identify a more potent dual TNF-α/IL-23 inhibitor
( ref………. Akama T, Antunes J, Freund Y, Kimura R, Dong C, Sanders V, et al. Structure-activity studies of novel oxaborole dual inhibitors of PDE4 and IL-23 release. 69th Annu Meet Soc Invest Dermatol (May 6-9, Montreal) 2009 Abst 282. ).
PATENT
WO 2007095638
https://www.google.co.in/patents/WO2007095638A2?cl=en
PATENT
WO 2006089067
http://www.google.co.in/patents/WO2006089067A2?cl=en
US 7582621
http://www.google.co.in/patents/US7582621
WO 2009111676
http://www.google.im/patents/WO2009111676A2?cl=en
WO 2007078340
http://www.google.im/patents/WO2007078340A2?cl=en
US 20070286822
http://www.google.com/patents/US20070286822
REFERENCES
1 Structure-activity studies led to the discovery of AN2898 in development for topical treatment of psoriasis and atopic dermatitis, J Am Acad Dermatol 2009, 60(3, Suppl. 1): Abst P1317
2 FEBS Letters (2012), 586(19), 3410-3414
/////////AN2898, AN 2898, ANACOR, BOROLE
B1(c2ccc(cc2CO1)Oc3ccc(c(c3)C#N)C#N)O
Filed under: Phase2 drugs, Uncategorized Tagged: AN 2898, AN2898, ANACOR, Borole, phase 2
