The activity of diguanidino and 'reversed' diamidino 2,5-diarylfurans versus Trypanosoma cruzi and Leishmania donovani.
The in vitro activity of 20 dicationic molecules containing either diguanidino or reversed amidine cationic groups were evaluated versus Trypanosoma cruzi and Leishmania donovani. The most active compounds were in the reversed amidine series and six exhibited IC(50) values of less than 1 micro mol versus T. cruzi and five gave similar values versus L. donovani.
Stephens
Chad E
CE
Department of Chemistry, Georgia State University, Atlanta, GA 30303-3083, USA. dboykin@gsu.edu
Brun
Reto
R
Salem
Manar M
MM
Werbovetz
Karl A
KA
Tanious
Farial
F
Wilson
W David
WD
Boykin
David W
DW
D000578:Amidines / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D004247:DNA / Q000378:metabolism; D005663:Furans / Q000737:chemistry* / Q000494:pharmacology*; D019791:Guanidine / Q000031:analogs & derivatives / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D007893:Leishmania donovani / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D008264:Macrophages / Q000187:drug effects; D009691:Nucleic Acid Denaturation; D009838:Oligodeoxyribonucleotides / Q000737:chemistry / Q000378:metabolism; D011067:Poly dA-dT / Q000737:chemistry / Q000378:metabolism; D015800:Protozoan Proteins / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship; D013696:Temperature; D014344:Trypanocidal Agents / Q000737:chemistry / Q000494:pharmacology; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000378:metabolism
D000578:Amidines; D005663:Furans; D009838:Oligodeoxyribonucleotides; D015800:Protozoan Proteins; D014344:Trypanocidal Agents; D011067:Poly dA-dT; D004247:DNA; D019791:Guanidine