Piperazine-linked bisbenzamidines: a novel class of antileishmanial agents.
A series of 13 1,4-diarylpiperazines has been prepared, evaluated for antileishmanial activity and their binding affinity to DNA was measured. Among these compounds, 1,4-bis[4-(1H-benzimidazol-2-yl)phenyl]piperazine (14) emerged as the most active compound with an IC(50) value of 0.41 microM which is about sevenfold more potent than pentamidine.
Mayence
Annie
A
Division of Basic Pharmaceutical Sciences, College of Pharmacy, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, LA 70125, USA.
Vanden Eynde
Jean Jacques
JJ
LeCour
Louis
L
Walker
Larry A
LA
Tekwani
Babu L
BL
Huang
Tien L
TL
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001665:Binding Sites; D002455:Cell Division / Q000187:drug effects*; D004247:DNA / Q000737:chemistry / Q000378:metabolism; D020128:Inhibitory Concentration 50; D007891:Leishmania / Q000187:drug effects*; D021261:Parasitic Sensitivity Tests; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000981:Antiprotozoal Agents; D010879:Piperazines; D004247:DNA