title: 2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase.
abstract: As part of our efforts aimed at searching for new antiparasitic agents, the effect of representative 2-alkylaminoethyl-1,1-bisphosphonic acids on Trypanosoma cruzi squalene synthase (TcSQS) was investigated. These compounds had proven to be potent inhibitors of T. cruzi. This cellular activity had been associated with an inhibition of the enzymatic activity of T. cruzi farnesyl diphosphate synthase. 2-Alkylaminoethyl-1,1-bisphosphonic acids appear to have a dual action, since they also inhibit TcSQS at the nanomolar range.
authors.affiliation: Instituto de Parasitología y Biomedicina López-Neyra, Consejo Superior de Investigaciones Científicas, Parque Tecnológico de Ciencias de la Salud, Granada, Spain.
authors.forename: Carlos A
authors.initials: CA
authors.lastname: Rodrígues-Poveda
authors.forename: Dolores
authors.initials: D
authors.lastname: González-Pacanowska
authors.forename: Sergio H
authors.initials: SH
authors.lastname: Szajnman
authors.forename: Juan B
authors.initials: JB
authors.lastname: Rodríguez
mesh_terms: D000977:Antiparasitic Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D014355:Chagas Disease / Q000188:drug therapy; D004164:Diphosphonates / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D013186:Farnesyl-Diphosphate Farnesyltransferase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D051228:Geranyltranstransferase / Q000037:antagonists & inhibitors*; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000201:enzymology* / Q000378:metabolism
chemical_list: D000977:Antiparasitic Agents; D004164:Diphosphonates; D014344:Trypanocidal Agents; D051228:Geranyltranstransferase; D013186:Farnesyl-Diphosphate Farnesyltransferase