Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters

Authors :: Erik Nielsen
Steffen Sinning
Søren V. Boye
Jeanette Willumsen
Mikael Bols
Ove Wiborg
Mikkel Due Petersen
Source :: Petersen, M D, Boye, S V, Nielsen, E H T, Willumsen, J, Bols, M, Sinning, S & Wiborg, O 2007, ' Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters ' Bioorganic and Medicinal Chemistry, vol. 15, no. 12, pp. 4159-4174 . https://doi.org/10.1016/j.bmc.2007.03.069, University of Copenhagen
Publication Year :: 2007
Abstract: A series of simple truncated analogues of phenyl tropanes, 2-arylcycloalk-1-enyl carboxylic acid methylesters, were prepared and investigated for their activity towards the dopamine, serotonin and norepinephrine transporters. The compounds were prepared from cyclic ketoesters, which were converted to enolic triflates and reacted with arylboronates using the Suzuki coupling. For comparison the corresponding piperidines were also made and investigated. The new compounds inhibit monoamine-transporters with Ki values ranging from 0.1 to 1000 μM.

Language :: English
Database :: OpenAIRE
Journal :: Petersen, M D, Boye, S V, Nielsen, E H T, Willumsen, J, Bols, M, Sinning, S & Wiborg, O 2007, ' Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters ' Bioorganic and Medicinal Chemistry, vol. 15, no. 12, pp. 4159-4174 . https://doi.org/10.1016/j.bmc.2007.03.069, University of Copenhagen
Accession number :: edsair.doi.dedup.....7aaec98a8697c227ee1a0d2f6a4533dc
Full Text :: https://doi.org/10.1016/j.bmc.2007.03.069

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