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  • Title: The influence of an ethylene spacer on the 5-HT(1A) and 5-HT(2A) receptor affinity of arylpiperazine derivatives of amides with N-acylated amino acids and 3-differently substituted pyrrolidine-2,5-diones.
    Author: Zajdel P, Subra G, Verdie P, Bojarski AJ, Duszyńska B, Basista K, Obniska J, Martinez J, Pawłowski M.
    Journal: Eur J Med Chem; 2009 Feb; 44(2):800-8. PubMed ID: 18603331.
    Abstract:
    A library of ethylene analogs of the previously described arylpiperazines with N-acylated amino acids was synthesized on SynPhase Lanterns and the library representatives were evaluated for their 5-HT(1A) and 5-HT(2A) receptor affinities. The obtained results were compared with those reported for compounds containing propylene and a butylene spacer and they revealed that 5-HT(1A) receptor affinity decreased proportionally with the length of the alkyl chain. Furthermore, the synthesized 3-cycloalkyl derivatives containing two methylene group spacers showed that the 3-position of pyrrolidine-2,5-dione preferred substituents of hydrophobic character.
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