Literature DB >> 22585217

2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase.

Carlos A Rodrígues-Poveda1, Dolores González-Pacanowska, Sergio H Szajnman, Juan B Rodríguez.   

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.

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Year:  2012        PMID: 22585217      PMCID: PMC3421570          DOI: 10.1128/AAC.00796-12

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN: 0066-4804            Impact factor:   5.191


  38 in total

1.  Structure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates.

Authors:  J E Dunford; K Thompson; F P Coxon; S P Luckman; F M Hahn; C D Poulter; F H Ebetino; M J Rogers
Journal:  J Pharmacol Exp Ther       Date:  2001-02       Impact factor: 4.030

2.  Bisphosphonates derived from fatty acids are potent growth inhibitors of Trypanosoma cruzi.

Authors:  S H Szajnman; B N Bailey; R Docampo; J B Rodriguez
Journal:  Bioorg Med Chem Lett       Date:  2001-03-26       Impact factor: 2.823

Review 3.  Specific chemotherapy of Chagas disease: controversies and advances.

Authors:  Julio A Urbina; Roberto Docampo
Journal:  Trends Parasitol       Date:  2003-11

4.  Trypanosoma cruzi contains major pyrophosphate stores, and its growth in vitro and in vivo is blocked by pyrophosphate analogs.

Authors:  J A Urbina; B Moreno; S Vierkotter; E Oldfield; G Payares; C Sanoja; B N Bailey; W Yan; D A Scott; S N Moreno; R Docampo
Journal:  J Biol Chem       Date:  1999-11-19       Impact factor: 5.157

5.  Synthesis and biological evaluation of new 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase.

Authors:  Valeria S Rosso; Sergio H Szajnman; Leena Malayil; Melina Galizzi; Silvia N J Moreno; Roberto Docampo; Juan B Rodriguez
Journal:  Bioorg Med Chem       Date:  2011-04-01       Impact factor: 3.641

6.  Bisphosphonates inhibit the growth of Trypanosoma brucei, Trypanosoma cruzi, Leishmania donovani, Toxoplasma gondii, and Plasmodium falciparum: a potential route to chemotherapy.

Authors:  M B Martin; J S Grimley; J C Lewis; H T Heath; B N Bailey; H Kendrick; V Yardley; A Caldera; R Lira; J A Urbina; S N Moreno; R Docampo; S L Croft; E Oldfield
Journal:  J Med Chem       Date:  2001-03-15       Impact factor: 7.446

Review 7.  Biology of Trypanosoma cruzi.

Authors:  Z Brener
Journal:  Annu Rev Microbiol       Date:  1973       Impact factor: 15.500

8.  In vivo activities of farnesyl pyrophosphate synthase inhibitors against Leishmania donovani and Toxoplasma gondii.

Authors:  Vanessa Yardley; Anis A Khan; Michael B Martin; Teri R Slifer; Fausto G Araujo; Silvia N J Moreno; Roberto Docampo; Simon L Croft; Eric Oldfield
Journal:  Antimicrob Agents Chemother       Date:  2002-03       Impact factor: 5.191

9.  Structural basis for bisphosphonate-mediated inhibition of isoprenoid biosynthesis.

Authors:  David J Hosfield; Yanming Zhang; Douglas R Dougan; Alexei Broun; Leslie W Tari; Ronald V Swanson; John Finn
Journal:  J Biol Chem       Date:  2003-12-12       Impact factor: 5.157

10.  Bisphosphonates derived from fatty acids are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase.

Authors:  Sergio H Szajnman; Andrea Montalvetti; Youhong Wang; Roberto Docampo; Juan B Rodriguez
Journal:  Bioorg Med Chem Lett       Date:  2003-10-06       Impact factor: 2.823

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  3 in total

1.  Activity of Fluorine-Containing Analogues of WC-9 and Structurally Related Analogues against Two Intracellular Parasites: Trypanosoma cruzi and Toxoplasma gondii.

Authors:  María N Chao; Catherine Li; Melissa Storey; Bruno N Falcone; Sergio H Szajnman; Sergio M Bonesi; Roberto Docampo; Silvia N J Moreno; Juan B Rodriguez
Journal:  ChemMedChem       Date:  2016-11-25       Impact factor: 3.466

2.  Genetic profiling of the isoprenoid and sterol biosynthesis pathway genes of Trypanosoma cruzi.

Authors:  Raúl O Cosentino; Fernán Agüero
Journal:  PLoS One       Date:  2014-05-14       Impact factor: 3.240

3.  High-Throughput Screening of the ReFRAME Library Identifies Potential Drug Repurposing Candidates for Trypanosoma cruzi.

Authors:  Jean A Bernatchez; Emily Chen; Mitchell V Hull; Case W McNamara; James H McKerrow; Jair L Siqueira-Neto
Journal:  Microorganisms       Date:  2020-03-26
  3 in total

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