Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain
R Nakajima, N Yamamoto, S Hirayama, T Iwai… - Bioorganic & Medicinal …, 2015 - Elsevier
We designed and synthesized pentacyclic propellane derivatives with a 6-amide side chain
to afford compounds with higher MOR/KOR ratio and lower sedative effects than nalfurafine.
The obtained etheno-bridged derivative with a β-amide side chain, YNT-854, showed a
higher MOR/KOR ratio than nalfurafine. YNT-854 also exhibited a higher dose ratio between
the sedative effect and the analgesic effect than observed with nalfurafine, which may guide
the future design of useful analgesics with a weaker sedative effect than nalfurafine.
to afford compounds with higher MOR/KOR ratio and lower sedative effects than nalfurafine.
The obtained etheno-bridged derivative with a β-amide side chain, YNT-854, showed a
higher MOR/KOR ratio than nalfurafine. YNT-854 also exhibited a higher dose ratio between
the sedative effect and the analgesic effect than observed with nalfurafine, which may guide
the future design of useful analgesics with a weaker sedative effect than nalfurafine.
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 3, novel propellane derivatives with pentacyclic skeletons
H Fujii, R Nakajima, J Akiyama, N Yamamoto… - Bioorganic & medicinal …, 2012 - Elsevier
Previously reported propellane derivative KNT-42 preferred the κ receptor and functioned as
a message part in the message-address concept, but its affinity for the κ receptor was not
high. To improve affinity, we synthesized five pentacyclic propellane derivatives designed for
the purpose of fixing the conformation of KNT-42. The etheno-and ethano-bridged
derivatives SYK-347 and SYK-393 exhibited high affinity and selectivity for the κ receptor,
whereas the other derivatives did not. These results would be due to the different ranges of …
a message part in the message-address concept, but its affinity for the κ receptor was not
high. To improve affinity, we synthesized five pentacyclic propellane derivatives designed for
the purpose of fixing the conformation of KNT-42. The etheno-and ethano-bridged
derivatives SYK-347 and SYK-393 exhibited high affinity and selectivity for the κ receptor,
whereas the other derivatives did not. These results would be due to the different ranges of …
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