4.7 Article

Synthesis, characterization and in vitro pharmacology of novel pregabalin derivatives

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 4, Pages 1447-1452

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2009.12.049

Keywords

Pregabalin; Gabapentin; Binding affinity

Funding

  1. Ministry of Science, Education and Sports of the Republic of Croatia [098-0982933-2908, 098-0982933-2936]

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A series of novel pregabalin derivatives were synthesized starting from N-protected pregabalin, different amino sugars, adamantylamine, serotonin and tryptamine. New compounds were spectroscopically characterized and in vitro tested on gabapentin receptor binding assay. The serotonin-pregabalin adduct showed significant binding effect and its IC(50) value was determined. (C) 2009 Elsevier Masson SAS. All rights reserved.

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