Short synthesis and antimalarial activity of fagaronine

M. Rivaud; A. Mendoza; M. Sauvain; A. Valentin; V. Jullian

doi:10.1016/j.bmc.2012.05.061

Short synthesis and antimalarial activity of fagaronine

M. Rivaud
, A. Mendoza
, M. Sauvain
, A. Valentin
, V. Jullian

Université de Toulouse
University of Navarra
Convenio IRD-PeruPetro

Producción científica: Contribución a una revista › Artículo › revisión exhaustiva

31 Citas (Scopus)

Resumen

Herein, we report a new synthesis of fagaronine 1, inspired by the synthesis reported by Luo for nornitidine. The in vitro biological activity of fagaronine against malaria on several chloroquine-sensitive and resistant Plasmodium falciparum strains was confirmed, and the selectivity index compared to mammalian cells was calculated. Fagaronine was found to have very good antimalarial activity in vivo, comparable to the activity of the reference compound chloroquine. Therefore, fagaronine appears to be a good potential lead for the design of new antimalarial molecules.

Idioma original	Inglés
Páginas (desde-hasta)	4856-4861
Número de páginas	6
Publicación	Bioorganic and Medicinal Chemistry
Volumen	20
N.º	15
DOI	https://doi.org/10.1016/j.bmc.2012.05.061
Estado	Publicada - 1 ago. 2012
Publicado de forma externa	Sí

ODS de las Naciones Unidas

Este resultado contribuye a los siguientes Objetivos de Desarrollo Sostenible

ODS 3: Salud y bienestar

Acceder al documento

10.1016/j.bmc.2012.05.061

Otros archivos y enlaces

Enlace a la publicación en Scopus

Citar esto

@article{5807984ad296433facc9a798f55bc3cd,

title = "Short synthesis and antimalarial activity of fagaronine",

abstract = "Herein, we report a new synthesis of fagaronine 1, inspired by the synthesis reported by Luo for nornitidine. The in vitro biological activity of fagaronine against malaria on several chloroquine-sensitive and resistant Plasmodium falciparum strains was confirmed, and the selectivity index compared to mammalian cells was calculated. Fagaronine was found to have very good antimalarial activity in vivo, comparable to the activity of the reference compound chloroquine. Therefore, fagaronine appears to be a good potential lead for the design of new antimalarial molecules.",

keywords = "Benzo[c]phenanthridine, Fagaronine, In vivo experiment, Malaria, Synthesis",

author = "M. Rivaud and A. Mendoza and M. Sauvain and A. Valentin and V. Jullian",

year = "2012",

month = aug,

day = "1",

doi = "10.1016/j.bmc.2012.05.061",

language = "Ingl{\'e}s",

volume = "20",

pages = "4856--4861",

journal = "Bioorganic and Medicinal Chemistry",

issn = "0968-0896",

number = "15",

}

TY - JOUR

T1 - Short synthesis and antimalarial activity of fagaronine

AU - Rivaud, M.

AU - Mendoza, A.

AU - Sauvain, M.

AU - Valentin, A.

AU - Jullian, V.

PY - 2012/8/1

Y1 - 2012/8/1

N2 - Herein, we report a new synthesis of fagaronine 1, inspired by the synthesis reported by Luo for nornitidine. The in vitro biological activity of fagaronine against malaria on several chloroquine-sensitive and resistant Plasmodium falciparum strains was confirmed, and the selectivity index compared to mammalian cells was calculated. Fagaronine was found to have very good antimalarial activity in vivo, comparable to the activity of the reference compound chloroquine. Therefore, fagaronine appears to be a good potential lead for the design of new antimalarial molecules.

AB - Herein, we report a new synthesis of fagaronine 1, inspired by the synthesis reported by Luo for nornitidine. The in vitro biological activity of fagaronine against malaria on several chloroquine-sensitive and resistant Plasmodium falciparum strains was confirmed, and the selectivity index compared to mammalian cells was calculated. Fagaronine was found to have very good antimalarial activity in vivo, comparable to the activity of the reference compound chloroquine. Therefore, fagaronine appears to be a good potential lead for the design of new antimalarial molecules.

KW - Benzo[c]phenanthridine

KW - Fagaronine

KW - In vivo experiment

KW - Malaria

KW - Synthesis

UR - https://www.scopus.com/pages/publications/84863988927

U2 - 10.1016/j.bmc.2012.05.061

DO - 10.1016/j.bmc.2012.05.061

M3 - Artículo

C2 - 22766218

AN - SCOPUS:84863988927

SN - 0968-0896

VL - 20

SP - 4856

EP - 4861

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 15

ER -

Short synthesis and antimalarial activity of fagaronine

Resumen

ODS de las Naciones Unidas

Acceder al documento

Otros archivos y enlaces

Huella

Citar esto