AustralieFrV1, Main, Exploration, bibRecord, 000315

Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.

Identifieur interne : 000315 ( Main/Exploration ); précédent : 000314; suivant : 000316

Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.

Auteurs : B. Sauer [Allemagne] ; T S Skinner-Adams [Australie] ; A. Bouchut [France] ; M J Chua [Australie] ; C. Pierrot [France] ; F. Erdmann [Allemagne] ; D. Robaa [Allemagne] ; M. Schmidt [Allemagne] ; J. Khalife [France] ; K T Andrews [Australie] ; W. Sippl [Allemagne]

Source :

European journal of medicinal chemistry [ 1768-3254 ] ; 2017.

RBID : pubmed:28038325

Descripteurs français

KwdFr :
- Antipaludiques (), Antipaludiques (pharmacologie), Antipaludiques (synthèse chimique), Antipaludiques (toxicité), Cellules Caco-2, Cellules HEK293, Conception de médicament, Furanes (), Furanes (pharmacologie), Furanes (synthèse chimique), Furanes (toxicité), Humains, Plasmodium falciparum (), Relation structure-activité, Techniques de chimie synthétique.
MESH :
- pharmacologie : Antipaludiques, Furanes.
- synthèse chimique : Antipaludiques, Furanes.
- toxicité : Antipaludiques, Furanes.
- Antipaludiques, Cellules Caco-2, Cellules HEK293, Conception de médicament, Furanes, Humains, Plasmodium falciparum, Relation structure-activité, Techniques de chimie synthétique.

English descriptors

KwdEn :
- Antimalarials (chemical synthesis), Antimalarials (chemistry), Antimalarials (pharmacology), Antimalarials (toxicity), Caco-2 Cells, Chemistry Techniques, Synthetic, Drug Design, Furans (chemical synthesis), Furans (chemistry), Furans (pharmacology), Furans (toxicity), HEK293 Cells, Humans, Plasmodium falciparum (drug effects), Structure-Activity Relationship.
MESH :
- chemical , chemical synthesis : Antimalarials, Furans.
- chemical , chemistry : Antimalarials, Furans.
- chemical , pharmacology : Antimalarials, Furans.
- chemical , toxicity : Antimalarials, Furans.
- drug effects : Plasmodium falciparum.
- Caco-2 Cells, Chemistry Techniques, Synthetic, Drug Design, HEK293 Cells, Humans, Structure-Activity Relationship.

Abstract

Malaria is one of the most significant tropical diseases and remains a major challenge due to the lack of a broadly effective vaccine and parasite resistance to current drugs. This means there is a need for new drug candidates with novel modes of action. Aromatic bisamidines, such as furamidine (DB75), were initially developed as anti-Trypanosoma agents however as clinical trials with furamidine highlighted potential side effects they were not pursued further in that setting. Despite apparent cytotoxicity liabilities the potency of furamidine against Plasmodium falciparum makes it a promising scaffold for the development of new anti-Plasmodium agents with improved selectivity. In this study a bisamidine compound series based on furamidine was synthesized by introducing modifications at the furan core structure and terminal amidine groups. The activity of the derived compounds was tested in vitro against drug sensitive and resistant P. falciparum lines and a human cell line (HEK293 cells) to generate anti-Plasmodium structure-activity relationships and to provide preliminary selectivity data.

DOI: 10.1016/j.ejmech.2016.12.041
PubMed: 28038325

Affiliations:

Allemagne, Australie, France

Le document en format XML

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<front><div type="abstract" xml:lang="en">Malaria is one of the most significant tropical diseases and remains a major challenge due to the lack of a broadly effective vaccine and parasite resistance to current drugs. This means there is a need for new drug candidates with novel modes of action. Aromatic bisamidines, such as furamidine (DB75), were initially developed as anti-Trypanosoma agents however as clinical trials with furamidine highlighted potential side effects they were not pursued further in that setting. Despite apparent cytotoxicity liabilities the potency of furamidine against Plasmodium falciparum makes it a promising scaffold for the development of new anti-Plasmodium agents with improved selectivity. In this study a bisamidine compound series based on furamidine was synthesized by introducing modifications at the furan core structure and terminal amidine groups. The activity of the derived compounds was tested in vitro against drug sensitive and resistant P. falciparum lines and a human cell line (HEK293 cells) to generate anti-Plasmodium structure-activity relationships and to provide preliminary selectivity data.</div>
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{{Explor lien
   |wiki=    Wicri/Asie
   |area=    AustralieFrV1
   |flux=    Main
   |étape=   Exploration
   |type=    RBID
   |clé=     pubmed:28038325
   |texte=   Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
}}

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Serveur d'exploration sur les relations entre la France et l'Australie

Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.

Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.

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Descripteurs français

English descriptors

Abstract

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	Serveur d'exploration sur les relations entre la France et l'Australie
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