Laboratory and industrial synthesis of remifentanil

Mathia, František; Marchalı́n, Štefan; Végh, Dániel; Bobošíková, Mária; Halinkovičová, Michaela

doi:10.2478/v10188-012-0022-2

Cited by 1 publication

(1 citation statement)

References 15 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A certain problem with 4-axial substituted fentanyl analogues is that they require multi-step and rather low-yielding syntheses. Notably however, some progress in their syntheses have been reported in several past years [ 124 , 125 , 126 , 127 ]. Moreover, in the field of mixed opioid ligands, there is an interesting recent example, in which carfentanil ( 1.2 ) fragments were hybridized with peptide dermorphine analogues to yield potent analgesics with improved properties [ 128 ].…”

Section: Discussionmentioning

confidence: 99%

Fentanyl Structure as a Scaffold for Opioid/Non-Opioid Multitarget Analgesics

Lipiński

Matalińska

2022

IJMS

View full text Add to dashboard Cite

One of the strategies in the search for safe and effective analgesic drugs is the design of multitarget analgesics. Such compounds are intended to have high affinity and activity at more than one molecular target involved in pain modulation. In the present contribution we summarize the attempts in which fentanyl or its substructures were used as a μ-opioid receptor pharmacophoric fragment and a scaffold to which fragments related to non-opioid receptors were attached. The non-opioid ‘second’ targets included proteins as diverse as imidazoline I2 binding sites, CB1 cannabinoid receptor, NK1 tachykinin receptor, D2 dopamine receptor, cyclooxygenases, fatty acid amide hydrolase and monoacylglycerol lipase and σ1 receptor. Reviewing the individual attempts, we outline the chemistry, the obtained pharmacological properties and structure-activity relationships. Finally, we discuss the possible directions for future work.

show abstract