70362-64-0

Upstream product

• 115255-87-3 4-trimethylsilyloxymethylphenol 
• 79-30-1 isobutyryl chloride 
• 126070-20-0 4-((tert-butyldimethylsilyloxy)methyl)phenol 
• 623-05-2 (4-hydroxyphenyl)methanol 
• 120464-79-1 4-formylphenyl isobutyrate 
• 1352347-92-2 C₁₇H₂₈O₃Si 
• 123-08-0 4-hydroxy-benzaldehyde 

Downstream Products

• 182878-05-3 4-(isopropylcarbonyl-oxy)benzyl iodide 
• 1346128-61-7 4-((((3-nitropyridin-4-yl)carbamoyl)oxy)methyl)phenyl isobutyrate 
• 1540917-76-7 C₃₁H₂₆O₅ 
• 151239-27-9 Bis(4-isobutyryloxybenzyl) N,N-diisopropylphosphoramidite 

Relevant academic research and scientific papers

Esterase-Triggered Self-Immolative Thiocarbamates Provide Insights into COS Cytotoxicity

Hydrogen sulfide (H2S) is an important gasotransmitter and biomolecule, and many synthetic small-molecule H2S donors have been developed for H2S-related research. One important class of triggerable H2S donors is

THIOETHER PRODRUG COMPOSITIONS AS ANTI-HIV AND ANTI-RETROVIRAL AGENTS

Disclosed are inhibitors of retroviral growth of formula (I), that are useful in treatment of retroviral infections such as HIV. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one compound or salt of the invention, a method for inactivating a virus, a method for dissociating a metal ion from a zinc finger-containing protein, and a method for inhibiting the transmission of a virus.

Formulating a new basis for the treatment against botulinum neurotoxin intoxication: 3,4-Diaminopyridine prodrug design and characterization

Botulism is a disease characterized by neuromuscular paralysis and is produced from botulinum neurotoxins (BoNTs) found within the Gram positive bacterium Clostridium botulinum. This bacteria produces the most deadliest toxin known, with lethal doses as low as 1 ng/kg. Due to the relative ease of production and transport, the use of these agents as potential bioterrorist weapons has become of utmost concern. No small molecule therapies against BoNT intoxication have been approved to date. However, 3,4-diaminopyridine (3,4-DAP), a potent reversible inhibitor of voltage-gated potassium channels, is an effective cholinergic agonist used in the treatment of neuromuscular degenerative disorders that require cholinergic enhancement. 3,4-DAP has also been shown to facilitate recovery of neuromuscular action potential post botulinum intoxication by blocking K+ channels. Unfortunately, 3,4-DAP displays toxicity largely due to blood-brain-barrier (BBB) penetration. As a dual-action prodrug approach to cholinergic enhancement we have designed carbamate and amide conjugates of 3,4-DAP. The carbamate prodrug is intended to be a slowly reversible inhibitor of acetylcholinesterase (AChE) along the lines of the stigmines thereby allowing increased persistence of released acetylcholine within the synaptic cleft. As a secondary activity, cleavage of the carbamate prodrug by AChE will afford the localized release of 3,4-DAP, which in turn, will enhance the pre-synaptic release of additional acetylcholine. Being a competitive inhibitor with respect to acetylcholine, the activity of the prodrug will be greatest at the synaptic junctions most depleted of acetylcholine. Here we report upon the synthesis and biochemical characterization of three new classes of prodrugs intended to limit previously reported stability and toxicity issues. Of the prodrugs examined, compound 32, demonstrated the most clinically relevant half-life of 2.76 h, while selectively inhibiting AChE over butyrylcholinesterase-a plasma-based high activity esterase. Future in vivo studies could provide validation of prodrug 32 as a potential treatment against BoNT intoxication as well as other neuromuscular disorders.

Bioreversible protection of nucleoside diphosphates

(Figure Presented) Going incognito: A new prodrug approach has been developed to facilitate the diffusion of highly polar polyphosphorylated nucleosides across cell membranes (see scheme). Inside the cell, the masking groups on the nucleoside diphosphate