155388-63-9

Upstream product

• 96-97-9 5-nitrosalicylic acid 
• 75-65-0 tert-butyl alcohol 
• 36805-97-7 N,N-dimethylformamide di-tert-butyl acetal 

Downstream Products

• 155388-93-5 5-aminosalicylic acid tert-butyl ester 
• 508210-93-3 tert-Butyl 2-benzhydryloxy-5-nitrobenzoate 
• 1422054-54-3 C₂₁H₂₄N₂O₅ 
• 1427469-69-9 tert-butyl 2-(2-ethoxy-2-oxoethoxy)-5-nitrobenzoate 
• 1427469-73-5 tert-butyl 5-(2,5-dimethyl-1H-pyrrol-1-yl)-2-(2-ethoxy-2-oxoethoxy)benzoate 
• 1427469-75-7 2-(2-(tert-butoxycarbonyl)-4-(2,5-dimethyl-1H-pyrrol-1-yl)phenoxy)acetic acid 
• 1427469-77-9 C₁₅H₁₅NO₅ 
• 1427469-71-3 C₁₅H₂₁NO₅ 
• 508211-74-3 tert-Butyl 2-[bis(4-fluorophenyl)methoxy]-5-nitrobenzoate 

Relevant academic research and scientific papers

BIFUNCTIONAL COMPOUNDS AND USE FOR REDUCING URIC ACID LEVELS

Bifunctional compounds that increase uric acid excretion and reduce uric acid production. Methods of using these compounds for reducing uric acid levels in blood or serum, for treating disorders of uric acid metabolism, and for maintaining normal uric acid levels in blood or serum are provided. Pharmaceutical compositions comprising the bifunctional compounds are also provided.

Design, synthesis, and biological evaluation of highly potent small molecule-peptide conjugates as new HIV-1 fusion inhibitors

The small molecule fusion inhibitors N-(4-carboxy-3-hydroxyphenyl)-2,5- dimethylpyrrole (NB-2) and N-(3-carboxy-4-hydroxyphenyl)-2,5-dimethylpyrrole (A12) target a hydrophobic pocket of HIV-1 gp41 and have moderate anti-HIV-1 activity. In this

Azo-reductase activated budesodine prodrugs for colon targeting

Budesodine is a synthetic glurocorticoid that undergoes substantial first pass metabolism, limiting systemic exposure. Its use in treatment of inflammatory bowel disease would benefit from a targeting strategy that could lead to a local topical effect, improving safety and increasing anti-inflammatory efficacy. A two-step prodrug strategy involving azoreduction/cyclization that we developed previously for prednisolone is here applied with some variations to budesonide. The budesodine prodrugs were tested using an in vitro azoreductase assay simulating human colonic microflora. The kinetics of amino steroid ester cyclization and its pH dependence was also evaluated. The stability of the prodrugs systems in simulated human duodenal and gastric fluid was evaluated to determine the likelihood of intact intestinal transit. The propionic acid derived prodrug 3 undergoes rapid activation by Clostridium perfingens and its putative reduction product cyclizes with acceptable rapidity when synthesized independently. These properties of 3 suggest that it has potential in management of ulcerative colitis.

TARGETING PRODRUGS AND COMPOSITIONS FOR THE TREATMENT OF GASTROINTESTINAL DISEASES

Provided herein are compounds, compositions and methods for preventing or treating gastrointestinal cancer in a mammal, wherein the method comprises delivering an effective amount of a COX-2 or a similar sulfonamide inhibitor as a prodrug or derivative thereof to the colon, wherein the COX-2 or similar inhibitor is released in- vivo.

TARGETING DIAZO PRODRUGS FOR THE TREATMENT OF GASTROINTESTINAL DISEASES

Provided herein are compounds, compositions and methods for decreasing NFkB DNA-binding activity in a patient comprising administering of a therapeutically effective amount of a compound or composition of the application to the patient to reduce, alleviate or treat various gastrointestinal diseases, such as inflammatory bowel disease (IBD).

Design, synthesis, and pharmacological effects of a cyclization-activated steroid prodrug for colon targeting in inflammatory bowel disease

Glucocorticoids are used in the treatment of inflammatory bowel disease. A limitation to their use is that they undergo absorption from the GIT before reaching the colon causing severe systemic side effects. We report here on a novel prodrug approach to targeting corticosteroids to the colon. The design involves attaching a 21-ester group that suppresses absorption during transit to the colon. The prodrug is designed to be primed by colonic microflora liberating an amino ester that cyclizes releasing the steroid. One of the prodrugs 5b was as efficacious as prednisolone in the murine DSS model but did not cause thymic atrophy, a marker for systemic steroid effects.

Structure-activity relationships in a series of 5-[(2,5- dihydroxybenzyl)amino]salicylate inhibitors of EGF-receptor-associated tyrosine kinase: Importance of additional hydrophobic aromatic interactions

Potent inhibitors of EGF-dependent protein tyrosine kinase (PTK) activity were synthesized in a series of 5-[(2,5-dihydroxybenzyl)amino]salicylates. Several of these compounds inhibited EGF-dependent DNA synthesis in ER 22 cells with IC50 1 μ