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

Research output: Contribution to journal › Article › peer-review

31 Scopus citations

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.

Original language	English
Pages (from-to)	4856-4861
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry
Volume	20
Issue number	15
DOIs	https://doi.org/10.1016/j.bmc.2012.05.061
State	Published - 1 Aug 2012
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Benzo[c]phenanthridine
Fagaronine
In vivo experiment
Malaria
Synthesis

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10.1016/j.bmc.2012.05.061

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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.",

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

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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

Abstract

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Keywords

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