New dual ligands for the D 2 and 5-HT 1A receptors from the group of 1,8-naphthyl derivatives of LCAP

More than 300 million people are suffering from depression, one of the civilization diseases in the 21st century. Serotonin 5-HT R and dopamine D R play an important role in the treatment and pathogenesis of depression. Moreover, in recent years, the efficacy of dual 5-HT /D receptors ligands has be...

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Published inBioorganic & medicinal chemistry letters Vol. 29; no. 16; p. 2236
Main Authors Zaręba, Przemysław, Jaśkowska, Jolanta, Śliwa, Paweł, Satała, Grzegorz
Format Journal Article
LanguageEnglish
Published England 15.08.2019
Subjects
Molecular modelling
5-HT(1A)/D
Serotonin receptors
Depression
Microwave-assisted
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Summary:More than 300 million people are suffering from depression, one of the civilization diseases in the 21st century. Serotonin 5-HT R and dopamine D R play an important role in the treatment and pathogenesis of depression. Moreover, in recent years, the efficacy of dual 5-HT /D receptors ligands has been demonstrated in the fight against depression. In this work the new bulky arylpiperazine derivatives (LCAP) were synthesized in microwave radiation field. The affinities for the selected serotonin (5-HT ,5-HT ,5-HT ,5-HT ) and dopamine (D ) receptors have been evaluated in vitro. Compounds 5.3a, 5.4, 5.1c, 5.3d, 5.2a are promising dual 5-HT R/D R ligands. The SAR analysis were additionally supported with molecular docking studies.
ISSN:1464-3405