1. Academic Validation
  2. Conjugation of l-NAME to prenyloxycinnamic acids improves its inhibitory effects on nitric oxide production

Conjugation of l-NAME to prenyloxycinnamic acids improves its inhibitory effects on nitric oxide production

  • Bioorg Med Chem Lett. 2013 May 15;23(10):2933-5. doi: 10.1016/j.bmcl.2013.03.050.
Salvatore Genovese 1 Francesco Epifano Serena Fiorito Massimo Curini Mariangela Marrelli Francesco Menichini Filomena Conforti
Affiliations

Affiliation

  • 1 Dipartimento di Farmacia, Università 'G. D'Annunzio' Chieti-Pescara, Via dei Vestini 31, 66100 Chieti Scalo (CH), Italy. s.genovese@unich.it
Abstract

A series of 10 compounds resulting from the conjugation of O-prenylated naturally occurring benzoic and cinnamic acids to l-NAME were synthesized and tested together with the corresponding unprenylated parent molecule as anti-inflammatory agents for their inhibitory effects on NO production in LPS-stimulated RAW 264.7 macrophages. Results indicated that the coupling between O-geranyl and O-isopentenylcinnamic acids and l-NAME led to products with an enhanced activity when compared to the parent compounds.

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