38376-29-3

Usage

Type of compound

Synthetic chemical compound

Mechanism of action

Potent and selective inhibitor of the enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)

Role in the body

Regulates the levels of steroid hormones

Potential therapeutic applications

Treatment of metabolic and endocrine disorders, including diabetes, obesity, and Cushing's syndrome

Current status

Under investigation for its therapeutic potential and may hold promise for the development of new and effective treatments for related conditions.

Upstream product

• 939909-89-4 2-acetylphenyl 2-fluorobenzoate 
• 90-02-8 salicylaldehyde 
• 445-27-2 2'-Fluoroacetophenone 
• 187173-68-8 2-[5-(2-Fluoro-phenyl)-3,4-dihydro-2H-pyrazol-3-yl]-phenol 

Relevant academic research and scientific papers

Decoupling Activation of Heme Biosynthesis from Anaerobic Toxicity in a Molecule Active in Staphylococcus aureus

Small molecules active in the pathogenic bacterium Staphylococcus aureus are valuable tools for the study of its basic biology and pathogenesis, and many molecules may provide leads for novel therapeutics. We have previously reported a small molecule, 1, which activates endogenous heme biosynthesis in S. aureus, leading to an accumulation of intracellular heme. In addition to this novel activity, 1 also exhibits toxicity towards S. aureus growing under fermentative conditions. To determine if these activities are linked and establish what features of the molecule are required for activity, we synthesized a library of analogs around the structure of 1 and screened them for activation of heme biosynthesis and anaerobic toxicity to investigate structure-activity relationships. The results of this analysis suggest that these activities are not linked. Furthermore, we have identified the structural features that promote each activity and have established two classes of molecules: activators of heme biosynthesis and inhibitors of anaerobic growth. These molecules will serve as useful probes for their respective activities without concern for the off target effects of the parent compound.

Structure-activity relationship studies of novel pyrazolo[1,5-c][1,3]benzoxazines: Synthesis and benzodiazepine receptor affinity

Some 2-arylpyrazolo[1,5-c][1,3]benzoxazin-5-ones 1 and 5 oxopyrazolo[1,5-c][1,3]benzoxazin-2-carboxylates 2 were prepared and biologically evaluated for their binding at benzodiazepine receptor (BZR) in rat cortical membranes. Structure-activity relations