Synthesis and pharmacological evaluation of sulfamide-based analogues of anandamide

  • Eur J Med Chem. 2009 Dec;44(12):4889-95. doi: 10.1016/j.ejmech.2009.08.003.
Carolina Cano  1 ,  Juan Antonio Páez ,  Pilar Goya ,  Antonia Serrano ,  Javier Pavón ,  Fernando Rodríguez de Fonseca ,  Margarita Suardíaz ,  María Isabel Martín
Affiliations
  • 1. Instituto de Química Médica, CSIC, Juan de la Cierva 3, Madrid 28006, Spain.
PMID: 19762126 DOI: 10.1016/j.ejmech.2009.08.003
Abstract

Arachidonyl and linoleyl sulfamide derivatives have been synthesized and their potential cannabimimetic properties evaluated in in vitro functional and binding assays. Replacement of the ethanolamide moiety of anandamide by -CH(2)NHSO(2)NH-R considerably reduces the CB1 receptor activity and only some of the compounds showed modest cannabinoid properties in binding assays. The new compounds were also tested as inhibitors of the FAAH enzyme but were inactive.

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