Antitrypanosomal activities of tryptanthrins.
New drugs and molecular targets are needed against Trypanosoma brucei, the protozoan that causes African sleeping sickness. Tryptanthrin (indolo[2,1-b]quinazoline-6,12-dione), a traditional antifungal agent, and 11 analogs were tested against T. brucei in vitro. The greatest activity was conferred by electron-withdrawing groups in the 8 position of the tryptanthrin ring system; the most potent compound had a 50% effective concentration of 0.40 microM.
Scovill
John
J
Department of Chemistry, Bucknell University, Lewisburg, Pennsylvania 17837, USA.
Blank
Elizabeth
E
Konnick
Michael
M
Nenortas
Elizabeth
E
Shapiro
Theresa
T
D000818:Animals; D002478:Cells, Cultured; D006801:Humans; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects
D011799:Quinazolines; D014344:Trypanocidal Agents; C046243:tryptanthrine