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bufexamac

别名 CP-1044-J3, Parfenac®, Paraderm®
Compound Class Synthetic organic
变动原因 In addition to inhibition of COX enzymes, this drug has been discovered to inhibit class IIb HDACs (ie HDACs 6 and 10) .

Summary

是否批准为药物?
IUPAC Name 2-(4-butoxyphenyl)-N-hydroxyacetamide
别名 CP-1044-J3, Parfenac®, Paraderm®

生物活性

生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
关联靶标 histone deacetylase 6 , histone deacetylase 10

临床资料

Summary of Clinical Use Bufexamac is a non-steroidal anti-inflammatory drug (NSAID). This drug was used to control the symptoms of inflammation of the skin (such as redness and itching) in diseases such as eczema and dermatitis. However, the EMA revoked marketing authorisation for medicines containing bufexamac throughout the European Union in 2010 due to an unacceptable risk of developing contact dermatitis. Other countries may still approve use of this drug.
作用机制与药效学效应 This drug was originally believed to primarily be a cyclooxygenase (COX) inhibitor, although its precise MMOA remains unclear . More recently, bufexamac has been discovered to inhibit HDACs 6 and 10, and subsequently inhibit IFN-α secretion , which may contribute to its anti-inflammatory action.

参考文献

1. Bantscheff M, Hopf C, Savitski MM, Dittmann A, Grandi P, Michon AM, Schlegl J, Abraham Y, Becher I, Bergamini G et al..  (2011)  Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes..  Nat Biotechnol,  29  (3):  (255-65).  [PMID:21258344]
2. Trommer H, Pl?tzer M, Raith K, Wohlrab W, Podhaisky HP, Neubert RH.  (2003)  Examinations of the antioxidative properties of the topically administered drug bufexamac reveal new insights into its mechanism of action..  J Pharm Pharmacol,  55  (10):  (1379-88).  [PMID:14607020]

结构

Canonical SMILES CCCCOc1ccc(cc1)CC(=O)NO
Isomeric SMILES CCCCOc1ccc(cc1)CC(=O)NO
InChI InChI=1S/C12H17NO3/c1-2-3-8-16-11-6-4-10(5-7-11)9-12(14)13-15/h4-7,15H,2-3,8-9H2,1H3,(H,13,14)
InChI key MXJWRABVEGLYDG-UHFFFAOYSA-N

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品牌简介

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