Synthesis and antimalarial activity of new haemanthamine-type derivatives

Juan C. Cedrón, David Gutiérrez, Ninoska Flores, Ángel G. Ravelo, Ana Estévez-Braun

Producción científica: Contribución a una revistaArtículorevisión exhaustiva

30 Citas (Scopus)

Resumen

Thirty one derivatives were prepared from the natural alkaloids haemanthamine (1), haemanthidine (2) and 11-hydroxyvittatine (3). They were evaluated for their in vitro antimalarial activity against chloroquine-sensitive strains of Plasmodium falciparum and some structure-activity relationships were outlined. For haemanthamine derivatives having a methoxy group at C-3, the presence of a free hydroxyl group at C-11 is important for the activity. The double bond at C-1-C-2 plays also an important role to achieve good inhibitory activity. Compound 35 with two nicotinate groups at C-3 and at C-11 was the most active compound with a IC50 = 0.8 ± 0.06 μM. © 2011 Elsevier Ltd. All rights reserved.
Idioma originalEspañol
Páginas (desde-hasta)5464-5472
Número de páginas9
PublicaciónBioorganic and Medicinal Chemistry
Volumen20
EstadoPublicada - 15 set. 2012
Publicado de forma externa

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