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Lancelot JC, Robba M, Bonnet JJ, Vaugeois JM, Costentin J.
“Synthesis and preliminary study of the activity of thiophene
analogues of pyrovalerone on the neuronal uptake of the monoamines”.
Eur J Med Chem. 1992;27:297-300.
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Abstract
Introduction
Application of the concept of benzene-thiophene isosterism
to structural changes led to an improvement in
the pharmaceutical profile of certain compounds
[l-6]. We have used this previously in the area of
spasmolytic or peripheral vasodilator activities with
P-substituted thiophene derivatives [7-91. In the
context of the investigation of substances with a
psychostimulant activity, and using the model of 2-Npyrrolidino-
1 -p-tolyl- 1 -pentanone (pyrovalerone) 1
[lO-141, we chose substitution of thiophene in 2 position
and studied a series of 2 amino-1-(2-thienyl)-lpentanones.
These aminoketones were evaluated in comparison
with pyrovalerone 1 with regard to their inhibition of
the monoamines (dopamine, norepinephrine, serotonine)
uptake and to the dopamine release by synaptosomal
preparations of rat brain.
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