943994-87-4

Usage

Uses

Used in Agriculture:
DIMBOA is used as a natural defense compound for plants to protect themselves against pests and pathogens. Its antimicrobial properties help in controlling the growth of harmful microorganisms, while its allelopathic properties enable it to inhibit the growth of competing plants.
Used in Medicine:
DIMBOA is used as a potential therapeutic agent due to its antioxidant properties. Its ability to neutralize free radicals and reduce oxidative stress makes it a promising candidate for the treatment of various diseases and conditions associated with oxidative stress, such as neurodegenerative disorders and cardiovascular diseases.
Used in Scientific Research:
DIMBOA is used as a subject of scientific research to further explore its potential uses and applications. Its unique structure and biological activities have attracted the interest of researchers, who are investigating its potential as a therapeutic agent, as well as its role in plant defense mechanisms.

Upstream product

• 121564-97-4 6-bromo-8-methyl-2H-1,4-benzoxazin-3(4H)-one 
• 73183-34-3 bis(pinacol)diborane 
• 943994-74-9 methyl (4-bromo-2-methyl-6-nitrophenoxy)acetate 
• 20294-50-2 4-bromo-2-methyl-6-nitrophenol 

Downstream Products

• 1221501-71-8 6-[1-(2,2-Difluoropropyl)-5-(4-fluorophenyl)-3-methyl-1H-pyrazol-4-yl]-8-methyl-2H-1,4-benzoxazin-3(4H)-one 
• 1221500-65-7 6-[5-(4-fluorophenyl)-1,3-dimethyl-1H-pyrazol-4-yl]-8-methyl-2H-1,4-benzoxazin-3(4H)-one 

Relevant academic research and scientific papers

Discovery of 6-[5-(4-fluorophenyl)-3-methyl-pyrazol-4-yl]-benzoxazin-3-one derivatives as novel selective nonsteroidal mineralocorticoid receptor antagonists

In the course of our study on selective nonsteroidal mineralocorticoid receptor (MR) antagonists, a series of novel benzoxazine derivatives possessing an azole ring as the core scaffold was designed for the purpose of attenuating the partial agonistic activity of the previously reported dihydropyrrol-2-one derivatives. Screening of alternative azole rings identified 1,3-dimethyl pyrazole 6a as a lead compound with reduced partial agonistic activity. Subsequent replacement of the 1-methyl group of the pyrazole ring with larger lipophilic side chains or polar side chains targeting Arg817 and Gln776 increased MR binding activity while maintaining the agonistic response at the lower level. Among these compounds, 6-[1-(2,2-difluoro-3-hydroxypropyl)-5-(4-fluorophenyl)-3-methyl-1H-pyrazol-4-yl]-2H-1,4-benzoxazin-3(4H)-one (37a) showed highly potent in vitro activity, high selectivity versus other steroid hormone receptors, and good pharmacokinetic profiles. Oral administration of 37a in deoxycorticosterone acetate-salt hypertensive rats showed a significant blood pressure-lowering effect with no signs of antiandrogenic effects.

FUSED HETEROCYCLIC COMPOUND AND USE THEREOF

The present invention relates to wherein each symbol is as defined in the specification. The compound has a superior mineral corticoidreceptorantagonistic action and is useful as an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like, a compound having a fused heterocycle, or a prodrug thereof, or a salt thereof; and an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like.