4.2 Article

Synthesis and biological investigations of 3β-aminotropane arylamide derivatives with atypical antipsychotic profile

期刊

MEDICINAL CHEMISTRY RESEARCH
卷 27, 期 8, 页码 1906-1928

出版社

SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-018-2203-z

关键词

Atypical antipsychotics; 3 beta-aminotropane derivatives; 5-HT1A, 5-HT2A, D-2; Dopamine receptor ligands

资金

  1. Jagiellonian University Medical College funds [K/ZDS/006133]

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This work is a continuation of our previous research, concentrating this time on lead structure modification to increase the 5-HT1A receptor affinity and water solubility of designed compounds. Therefore, the compounds synthesised within the present project included structural analogues of 3 beta-acylamine derivatives of tropane with the introduction of a methyl substituent in the benzyl ring and a 2-quinoline, 3-quinoline, or 6-quinoline moiety. A series of novel 3 beta-aminotropane derivatives was evaluated for their affinity for 5-HT1A, 5-HT2A, and D-2 receptors, which allowed for the identification of compounds 12e, 12i, and 19a as ligands with highest affinity for the tested receptors; they were then subjected to further evaluation in preliminary in vivo studies. Selected compounds 12i and 19a displayed antipsychotic properties in the d-amphetamine-induced and MK-801-induced hyperlocomotor activity test in mice. Moreover, compound 19a showed significant antidepressant-like activity in the forced swim test in mice.

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