Novel bisbenzimidazoles with antileishmanial effectiveness.
A small library of 2,2'-[(alpha,omega-alkanediylbis(oxyphenylene)]bis-1H-benzimidazoles has been prepared and screened in vitro against Pneumocystis carinii, Trypanosoma brucei rhodesiense, and Leishmania donovani. Among the six tested compounds two derivatives emerged as promising hits characterized by IC(50) values lower than that determined for pentamidine against L. donovani.
Mayence
Annie
A
Xavier University of Louisiana, College of Pharmacy, Division of Basic Pharmaceutical Sciences, 1 Drexel Drive, New Orleans, LA 70125, USA.
Pietka
Aurélie
A
Collins
Margaret S
MS
Cushion
Melanie T
MT
Tekwani
Babu L
BL
Huang
Tien L
TL
Vanden Eynde
Jean Jacques
JJ
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006690:Bisbenzimidazole / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007893:Leishmania donovani / Q000187:drug effects; D015394:Molecular Structure; D045363:Pneumocystis carinii / Q000187:drug effects; D013329:Structure-Activity Relationship; D014346:Trypanosoma brucei brucei / Q000187:drug effects
D000981:Antiprotozoal Agents; D006690:Bisbenzimidazole