- New Arylpiperazinylalkyl Derivatives of 8-Alkoxy-purine-2,6-dione and Dihydro[1,3]oxazolo[2,3-f]purinedione Targeting the Serotonin 5-HT1A/5-HT2A/5-HT7 and Dopamine D2 Receptors
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To obtain potential antidepressants and/or antipsychotics, a series of new long-chain arylpiperazine derivatives of 8-alkoxy-purine-2,6-dione (10-24) and dihydro[1,3]oxazolo[2,3-f]purinedione (30-34) were synthesized and their serotonin (5-HT1A, 5-HT2A, 5-HT6, 5-HT7) and dopamine (D2) receptor affinities were determined. The study allowed the identification of some potent 5-HT1A/5-HT7/D2 ligands with moderate affinity for 5-HT2A sites. The binding mode of representative compounds from both chemical classes (11 and 31) in the site of 5-HT1A receptor was analyzed in computational studies. In functional in vitro studies, the selected compounds 15 and 16 showed antagonistic properties for the evaluated receptors. 8-Methoxy-7-{4-[4-(2-methoxyphenyl)-piperazin-1-yl]-butyl}-1,3-dimethyl-purine-2,6-dione (15) showed a lack of activity in terms and under the conditions of the forced swim, four plate and amphetamine-induced hyperactivity tests in mice, probably as a result of its high first pass effect in the liver.
- Ch?oń-Rzepa, Grazyna,Zagórska, Agnieszka,Bucki, Adam,Ko?aczkowski, Marcin,Paw?owski, Maciej,Sata?a, Grzegorz,Bojarski, Andrzej J.,Partyka, Anna,Weso?owska, Anna,P?kala, Elzbieta,S?oczyńska, Karolina
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p. 242 - 253
(2015/04/14)
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- 9-(Piperazinylalkyl)carbazoles as Bax-modulators
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The present invention is related to piperazine derivatives of carbazole notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such piperazine derivatives of carbazole. Said piperazine derivatives of car
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- Synthesis and antidepressant activity of 5-(1-aryl-4-piperazino)methyl-2-amino-2-oxazolines
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The synthesis of 20 5-(1-aryl-4-piperazino)methyl-2-amino-2-oxazolines is described. Antidepressant activity was observed in mice using classical screening tests. Structure-activity relationships were studied and correlated with the nature of the aromatic
- Bosc,Jarry,Carpy,Panconi,Descas
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p. 437 - 442
(2007/10/02)
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