Reverse-benzamidine antimalarial agents : Design, synthesis, and biological evaluation

Olivier Berger; Sharon Wein; Jean-Frédéric Duckert; Marjorie Maynadier; Siham El Fangour; Roger Escale; Thierry Durand; Henri Vial; Yen Vo-Hoang

doi:10.1016/j.bmcl.2010.07.124

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Reverse-benzamidine antimalarial agents : Design, synthesis, and biological evaluation

Journal article

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Peer reviewed

Reverse-benzamidine antimalarial agents : Design, synthesis, and biological evaluation

Olivier Berger, Sharon Wein, Jean-Frédéric Duckert, Marjorie Maynadier, Siham El Fangour, Roger Escale, Thierry Durand, Henri Vial and Yen Vo-Hoang

Bioorganic and Medicinal Chemistry Letters, Vol.20(19), pp.5815-5817

14/06/2010

DOI: https://doi.org/10.1016/j.bmcl.2010.07.124

Abstract

Reverse-benzamidines

Chemical design

Bis-N-akylamidines

Antimalarial agents

Total clearance of parasitemia

In the frame of the development of bis-cationic choline analogs, the RSA of bis-N-alkylamidines were studied and a new series of reverse-benzamidine derivatives was designed. Contrary to the lipophilicity, the basicity of alkylamidine compounds directly influences their antimalarial potencies.

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Title: Reverse-benzamidine antimalarial agents : Design, synthesis, and biological evaluation
Creators - without role: Olivier Berger - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Sharon Wein - Université de Montpellier, Laboratory of Pathogens and Host Immunity - LPHI
Jean-Frédéric Duckert - Dynamique moléculaire des interactions membranaires
Marjorie Maynadier - Université de Montpellier, Laboratory of Pathogens and Host Immunity - LPHI
Siham El Fangour - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Roger Escale - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Thierry Durand - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Henri Vial - Université de Montpellier, Laboratory of Pathogens and Host Immunity - LPHI
Yen Vo-Hoang - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Publication Details: Bioorganic and Medicinal Chemistry Letters, Vol.20(19), pp.5815-5817
Identifiers: 9942970909311
Academic Unit: Laboratory of Pathogens and Host Immunity - LPHI; Institut des Biomolécules Max Mousseron - IBMM
Language: English
Resource Type: Journal article
Local Fields: hal-00517092