title: Bisphosphonates derived from fatty acids are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase.
abstract: Studies on the mode of action of a series of bisphosphonates derived from fatty acids, which had previously proved to be potent inhibitors against Trypanosoma cruzi proliferation in in vitro assays, have been performed. Some of these drugs proved to be potent inhibitors against the intracellular form of the parasite, exhibiting IC(50) values at the low micromolar level. As bisphosphonates are FDA clinically approved for treatment of bone resorption disorders, their potential innocuousness makes them good candidates to control tropical diseases.
authors.affiliation: Departamento de Química Orgánica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, C1428EHA Buenos Aires, Argentina.
authors.forename: Sergio H
authors.initials: SH
authors.lastname: Szajnman
authors.forename: Andrea
authors.initials: A
authors.lastname: Montalvetti
authors.forename: Youhong
authors.initials: Y
authors.lastname: Wang
authors.forename: Roberto
authors.initials: R
authors.lastname: Docampo
authors.forename: Juan B
authors.initials: JB
authors.lastname: Rodriguez
mesh_terms: D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D000818:Animals; D004164:Diphosphonates / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D005227:Fatty Acids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D051228:Geranyltranstransferase; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000201:enzymology
chemical_list: D004164:Diphosphonates; D004791:Enzyme Inhibitors; D005227:Fatty Acids; D019883:Alkyl and Aryl Transferases; D051228:Geranyltranstransferase