770710-46-8

Upstream product

• 1256354-61-6 1-(4-ethylphenyl)-3-(2-hydroxy-5-nitrophenyl)thiourea 
• 99-57-0 2-hydroxy-5-nitroaniline 
• 18856-63-8 (4-ethylphenyl)isothiocyanate 

Downstream Products

• 1352429-18-5 N²-(4-ethylphenyl)benzo[d]oxazole-2,5-diamine 
• 1352429-19-6 N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)-2-phenylacetamide 
• 1352429-32-3 N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)-4-heptylbenzamide 
• 1352429-31-2 N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)-3,4,5-trimethoxybenzamide 
• 1352429-29-8 N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)-4-tert-butylbenzamide 
• 1352429-28-7 2-ethoxy-N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)benzamide 
• 1352429-27-6 N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)-3-fluoro-5-(trifluoromethyl)benzamide 
• 1352429-26-5 4-ethyl-N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)benzamide 
• 1352429-25-4 3-(chloromethyl)-N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)benzamide 
• 1352429-24-3 3,4-dichloro-N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)benzamide 
• 1352429-23-2 2-chloro-N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)-5-nitrobenzamide 
• 1352429-22-1 2-chloro-N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)-4-nitrobenzamide 
• 1352429-21-0 4-chloro-N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)benzamide 
• 1352429-20-9 N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)benzamide 

Relevant academic research and scientific papers

5-Lipoxygenase inhibitors suppress RANKL-induced osteoclast formation via NFATc1 expression

5-Lipoxygenase synthesizes leukotrienes from arachidonic acid. We developed three novel 5-LO inhibitors having a benzoxazole scaffold as a potential anti-osteoclastogenics. They significantly suppressed RANKL-induced osteoclast formation in mouse bone marrow-derived macrophages. Furthermore, one compound, K7, inhibited the bone resorptive activity of osteoclasts. The anti-osteoclastogenic effect of K7 was mainly attributable to reduction in the expression of NFATc1, an essential transcription factor for osteoclast differentiation. K7 inhibited osteoclast formation via ERK and p38 MAPK, as well as NF-κB signaling pathways. K7 reduced lipopolysaccharide (LPS)-induced osteoclast formation in vivo, corroborating the in vitro data. Thus, K7 exerted an inhibitory effect on osteoclast formation in vitro and in vivo, properties that make it a potential candidate for the treatment of bone diseases associated with excessive bone resorption.

New compounds, the preparation thereof and pharmaceutical composition comprising the same for alleviation, prevention or treatment of osteoporosis

PURPOSE: A novel compound and a composition containing the same for preventing or treating osteoporosis are provided to suppress osteoclast formulation and bone resorption and to be used as an agent for relieving, preventing, or treating osteoporosis. CONSTITUTION: A novel compound which relieves, prevents, or treats osteoporosis is denoted by chemical formula I. A method for preparing the compound of chemical formula I comprises: a step of reacting a compound of chemical formula II and 5-bromoveleric acid by amide bond under the presence of PyBOP(benzotriazo l-1-yl-oxytripyrrolidinophosphonium hexafluorophosphate) and tertiary amine to prepare a compound of chemical formula III; and a step of reacting the compound of chemical formula III with a compound of chemical formula IV under the presence of a base. The tertiary amine includes triethyl amine, N,N-diisopropyl ethyl amine, N-methyl pyperidine, 4-dimethyl amino pyridine, N,N-dimethyl anline, 2,6-lutidine, or pyridine. The base is sodium carbonate, potassium carbonate, calcium carbonate, or sodium phosphate. A pharmaceutical composition for relieving, preventing, or treating osteoporosis contains the novel compounds, pharmaceutically acceptable salt thereof, or hydrate, or solvate thereof.

Synthesis of benzoxazole derivatives as interleukin-6 antagonists

A growing number of studies have demonstrated that interleukin (IL)-6 plays pathological roles in the development of chronic inflammatory disease and autoimmune disease by activating innate immune cells and by stimulating adaptive inflammatory T cells. So, suppression of IL-6 function may be beneficial for prevention and treatment of chronic inflammatory disease. This study reports that a series of synthetic derivatives of benzoxazole have suppressive effects on IL-6-mediated signaling. Among 16 synthetic derivatives of benzoxazole, the compounds 4, 6, 11, 15, 17, and 19 showed a strong suppressive activity against IL-6-induced phosphorylation of signal transducer and activator of transcription (STAT) 3 by 80–90%. While the cell viability was strongly decreased by compounds 11, 17, 19, the compounds 4, 6, and 15 revealed less cytotoxicity. We then examined the effects of the compounds on inflammatory cytokine production by CD4+ T cells. CD4+ T cells were induced to differentiate into interferon (IFN)-γ-, IL-17-, or IL-4-producing effector T cells in the presence of either the compound 4 or the compound 7. While the inactive compound 7 had no significant effect on the cytokine production by effector T cells, the active compound 4 strongly suppressed the production of inflammatory cytokines IFN-γ and IL-17, and also inhibited allergic inflammatory cytokines IL-4, IL-5, and IL-13 produced by effector Th2 cells. These results suggest that a benzoxazole derivative, compound 4 effectively suppresses IL-6-STAT3 signaling and inflammatory cytokine production by T cells and provides a beneficial effect for treating chronic inflammatory and autoimmune disease.

Benzoxazole Derivatives Having Inhibitory Activity Against Interleukin-6, Preparation Method Thereof, and Pharmaceutical Composition Containing the Same

The present invention relates to benzoxazole derivatives represented by the Formula 1, which has an inhibitory activity against interleukin-6 (IL-6), a method for preparation thereof, and a pharmaceutical composition containing the same. The compound represented by the Formula 1 according to the present invention has a superior inhibitory activity against interleukin-6, and therefore, can be practically applied for prevention and treatment of diseases caused by abnormal interleukin-6 activity.

Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors

5-Lipoxygenase (5-LOX) is important enzyme in the biosynthesis of leukotrienes, and is a potential target in the treatment of asthma and allergy. We designed and synthesized a series of benzoxazoles and benzothiazoles as 5-LOX inhibitors. Fourteen compoun