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Title

Synthesis and antileishmanial activity of C7- and C12-functionalized dehydroabietylamine derivatives.

AuthorsDea-Ayuela, M. Auxiliadora; Bilbao-Ramos, Pablo; Bolás-Fernández, Francisco; González-Cardenete, Miguel A.
KeywordsLeishmanicidal
Abietane
Diterpene
Dehydroabietylamine
Issue Date4-Oct-2016
PublisherElsevier
AbstractAbietane-type diterpenoids, either naturally occurring or synthetic, have shown a wide range of pharmacological actions, including antiprotozoal properties. In this study, we report on the antileishmanial evaluation of a series of (+)-dehydroabietylamine derivatives functionalized at C7 and/or C12. Thus, the activity in vitro against Leishmania infantum, Leishmania donovani, Leishmania amazonensis and Leishmania guyanensis, was studied. Most of the benzamide derivatives showed activities at low micromolar concentration against cultured promastigotes of Leishmania spp. (IC50 = 2.2–46.8 μM), without cytotoxicity on J774 macrophage cells. Compound 15, an acetamide, was found to be the most active leishmanicidal agent, though it presented some cytotoxicity on J774 cells. Among the benzamide derivatives, compounds 8 and 10, were also active against L. infantum intracellular amastigotes, being 18- and 23-fold more potent than the reference compound miltefosine, respectively. Some structure-activity relationships have been identified for the antileishmanial activity in these dehydroabietylamine derivatives.
URIhttp://hdl.handle.net/10261/164469
DOIhttps://doi.org/10.1016/j.ejmech.2016.06.004
ISSN0223-5234
E-ISSN1768-3254
Appears in Collections:(ITQ) Artículos
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