Bisphosphonates derived from fatty acids are potent growth inhibitors of Trypanosoma cruzi.
We have investigated the effect of a series of bisphosphonates derived from fatty acids against Trypanosoma cruzi proliferation in in vitro assays. Some of these drugs proved to be potent inhibitors against the intracellular form of the parasite exhibiting IC50 values at the low micromolar level. As bisphosphonates are FDA clinically approved for treatment of bone resorption, their potential innocuousness makes them good candidates to control tropical diseases.
Szajnman
S H
SH
Departamento de Química Orgánica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, Argentina.
Bailey
B N
BN
Docampo
R
R
Rodriguez
J B
JB
D000818:Animals; D001862:Bone Resorption / Q000188:drug therapy; D004164:Diphosphonates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D005227:Fatty Acids / Q000737:chemistry*; D006801:Humans; D020128:Inhibitory Concentration 50; D021261:Parasitic Sensitivity Tests; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000254:growth & development; D014481:United States; D014486:United States Food and Drug Administration
D004164:Diphosphonates; D005227:Fatty Acids; D014344:Trypanocidal Agents