The influence of catalyst in reaction 4360-63-8

Here is a brief introduction to this compound(4360-63-8)Electric Literature of C4H7BrO2, if you want to know about other compounds related to this compound(4360-63-8), you can read my other articles.

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Sulfide analogues of flupirtine and retigabine with nanomolar KV7.2/KV7.3 channel opening activity, published in 2019, which mentions a compound: 4360-63-8, mainly applied to flupirtine retigabine potassium channel; KCNQ; KV7; flupirtine; retigabine; sulfides, Electric Literature of C4H7BrO2.

The potassium channel openers flupirtine and retigabine have proven to be valuable analgesics or antiepileptics. Their recent withdrawal due to occasional hepatotoxicity and tissue discoloration, resp., leaves a therapeutic niche unfilled. Metabolic oxidation of both drugs gives rise to the formation of electrophilic quinones. These elusive, highly reactive metabolites may induce liver injury in the case of flupirtine and blue tissue discoloration after prolonged intake of retigabine. We examined which structural features can be altered to avoid the detrimental oxidation of the aromatic ring and shift oxidation toward the formation of more benign metabolites. Structure-activity relationship studies were performed to evaluate the KV7.2/3 channel opening activity of 45 derivatives Sulfide analogs were identified that are devoid of the risk of quinone formation, but possess potent KV7.2/3 opening activity. For example, flupirtine analog 3-(3,5-difluorophenyl)-N-(6-(isobutylthio)-2-(pyrrolidin-1-yl)pyridin-3-yl)propanamide (48) has 100-fold enhanced activity (EC50=1.4 nM), a vastly improved toxicity/activity ratio, and the same efficacy as retigabine in vitro.

Here is a brief introduction to this compound(4360-63-8)Electric Literature of C4H7BrO2, if you want to know about other compounds related to this compound(4360-63-8), you can read my other articles.

Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem