Reverse-benzamidine antimalarial agents: design, synthesis, and biological evaluation.
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.
Berger
Olivier
O
Institut des Biomolécules Max Mousseron UMR 5247 CNRS-Universités Montpellier I et II, Faculté de Pharmacie, 15 Av Ch Flahault, 34093 Montpellier cedex 5, France.
Wein
Sharon
S
Duckert
Jean-Frederic
JF
Maynadier
Marjorie
M
El Fangour
Siham
S
Escale
Roger
R
Durand
Thierry
T
Vial
Henri
H
Vo-Hoang
Yen
Y
D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001550:Benzamidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
D000962:Antimalarials; D001550:Benzamidines