59611-57-3

Upstream product

• 1140-81-4 N-(4-hydroxy-2-methylquinolin-6-yl)acetamide 
• 122-80-5 N-acetyl-p-phenylenediamine 
• 1131-34-6 6-amino-2-methylquinolin-4-ol 
• 500349-72-4 1-(4-chloro-2-methyl-[6]quinolyl)-ethanone 
• 500349-77-9 1-(4-hydroxy-2-methyl-[6]quinolyl)-ethanone 
• 63304-45-0 (E)-ethyl 3-((4-acetamidophenyl)amino)but-2-enoate 

Downstream Products

• 60504-61-2 N,N'-bis-(6-amino-2-methyl-[4]quinolyl)-hexanediyldiamine 
• 100795-23-1 N-(4-methoxy-2-methyl-6-quinolyl)acetamide 

Relevant academic research and scientific papers

Amide derivatives and nociceptin antagonists

The present invention relates to a compound of the formula [1′] wherein R2is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the like, E is a single bond, —O—, —S— and the like, ring G is aryl, heterocyclic group and the like, R5is halogen atom, hydroxy, lower alkyl optionally substituted by halogen atom etc., and the like, t is 0 or an integer of 1 to 5, when t is an integer of 2 to 5, each R5may be the same or different, m is 0 or an integer of 1 to 8, and n is 0 or an integer of 1 to 4, and a nociceptin antagonist containing compound [1′] as an active ingredient. The compound [1′] shows, due to nociceptin antagonistic action, analgesic effect against sharp pain such as postoperative pain and the like. The present invention also relates to the use of certain amide derivative inclusive of compound [1′] as a nociceptin antagonist or analgesic.

4-Aminoquinolines: Novel nociceptin antagonists with analgesic activity

Small-molecule nociceptin antagonists were synthesized to examine their therapeutic potential. After a 4-aminoquinoline derivative was found to bind with the human ORL1 receptor, a series of 4-aminoquinolines and related compounds were synthesized and their binding was evaluated. Elucidation of structure - Activity relationships eventually led to the optimum compounds. One of these compounds, N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide hydrochloride (11) not only antagonized nociceptin-induced allodynia in mice but also showed analgesic effect in a hot plate test using mice and in a formalin test using rats. Its analgesic effect was not antagonized by the opioid antagonist naloxone. These results indicate that this nociceptin antagonist has the potential to become a novel type of analgesic that differs from μ-opioid agonists.