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Synthesis and In Vitro Evaluation of Novel Dopamine Receptor D 2 3,4-dihydroquinolin-2(1 H )-one Derivatives Related to Aripiprazole
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Synthesis and In Vitro Evaluation of Novel Dopamine Receptor D 2 3,4-dihydroquinolin-2(1 H )-one Derivatives Related to Aripiprazole
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Synthesis and In Vitro Evaluation of Novel Dopamine Receptor D 2 3,4-dihydroquinolin-2(1 H )-one Derivatives Related to Aripiprazole
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Journal Article
Synthesis and In Vitro Evaluation of Novel Dopamine Receptor D 2 3,4-dihydroquinolin-2(1 H )-one Derivatives Related to Aripiprazole
2021
Overview
In this pilot study, a series of new 3,4-dihydroquinolin-2(1
)-one derivatives as potential dopamine receptor D
(D
R) modulators were synthesized and evaluated in vitro. The preliminary structure-activity relationship disclosed that compound
exhibited the highest D
R affinity among the newly synthesized compounds. In addition,
showed a very low cytotoxic profile and a high probability to cross the blood-brain barrier, which is important considering the observed affinity. However, molecular modelling simulation revealed completely different binding mode of
compared to USC-D301, which might be the culprit of the reduced affinity of
toward D
R in comparison with USC-D301.
