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

ABSTRACT: This work is a continuation of our previous research, concentrating this time on lead structure modification to increase the 5-HT_1A receptor affinity and water solubility of designed compounds. Therefore, the compounds synthesised within the present project included structural analogues of 3β-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 3β-aminotropane derivatives was evaluated for their affinity for 5-HT_1A, 5-HT_2A, and D₂ 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 e

SUBMITTER: Stefanowicz J 

PROVIDER: S-EPMC6061170 | biostudies-literature | 2018

REPOSITORIES: biostudies-literature