Structure–activity relationships of 6-(aminomethylphenoxy)-benzoxaborole derivatives as anti-inflammatory agent

Bioorganic & Medicinal Chemistry Letters
2013.0

Abstract

A series of novel 6-(aminomethylphenoxy)benzoxaborole analogs was synthesized for the investigation of the structure-activity relationship of the inhibition of TNF-alpha, IL-1beta, and IL-6, from lipopolysaccharide stimulated peripheral blood mononuclear cells. Compounds 9d and 9e showed potent activity against all three cytokines with IC50 values between 33 and 83nM. Chloro substituted analog 9e (AN3485) is considered to be a promising lead for novel anti-inflammatory agent with a favorable pharmacokinetic profile.

Knowledge Graph

Similar Paper

Structure–activity relationships of 6-(aminomethylphenoxy)-benzoxaborole derivatives as anti-inflammatory agent
Bioorganic & Medicinal Chemistry Letters 2013.0
Discovery and structure–activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis
Bioorganic & Medicinal Chemistry Letters 2009.0
Synthesis and anti-inflammatory activity evaluation of a novel series of 6-phenoxy-[1,2,4]triazolo[3,4- a ]phthalazine-3-carboxamide derivatives
Bioorganic & Medicinal Chemistry Letters 2016.0
Analogues of boswellic acids as inhibitors of pro-inflammatory cytokines TNF-α and IL-6
Bioorganic & Medicinal Chemistry Letters 2016.0
First synthesis and biological evaluation of 4-amino-2-aryl-6,9-dichlorobenzo[g]pteridines as inhibitors of TNF-α and IL-6
European Journal of Medicinal Chemistry 2013.0
Design, synthesis, characterization and biological evaluation of novel pyrazole integrated benzophenones
Bioorganic & Medicinal Chemistry Letters 2013.0
TNF-α and IL-6 inhibitors: Conjugates of N-substituted indole and aminophenylmorpholin-3-one as anti-inflammatory agents
European Journal of Medicinal Chemistry 2017.0
Synthesis of 6-aminomethyl derivatives of benzopyran-4-one with dual biological properties: Anti-inflammatory-analgesic and antimicrobial
European Journal of Medicinal Chemistry 2009.0
Design, synthesis, biological evaluation, and molecular docking of chalcone derivatives as anti-inflammatory agents
Bioorganic & Medicinal Chemistry Letters 2017.0
Synthesis of Novel Tylophorine Derivatives and Evaluation of Their Anti-Inflammatory Activity
ACS Medicinal Chemistry Letters 2014.0