Literature DB >> 12951099

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

Sergio H Szajnman1, Andrea Montalvetti, Youhong Wang, Roberto Docampo, Juan B Rodriguez.   

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.

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Year:  2003        PMID: 12951099     DOI: 10.1016/s0960-894x(03)00663-2

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  19 in total

1.  Farnesyl diphosphate synthase localizes to the cytoplasm of Trypanosoma cruzi and T. brucei.

Authors:  Marcela Ferella; Zhu-Hong Li; Björn Andersson; Roberto Docampo
Journal:  Exp Parasitol       Date:  2008-03-13       Impact factor: 2.011

2.  Binding of nitrogen-containing bisphosphonates (N-BPs) to the Trypanosoma cruzi farnesyl diphosphate synthase homodimer.

Authors:  Chuan-Hsiang Huang; Sandra B Gabelli; Eric Oldfield; L Mario Amzel
Journal:  Proteins       Date:  2010-03

3.  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

4.  Synthesis and biological evaluation of 1-alkylaminomethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii.

Authors:  Tamila Galaka; Bruno N Falcone; Catherine Li; Sergio H Szajnman; Silvia N J Moreno; Roberto Docampo; Juan B Rodriguez
Journal:  Bioorg Med Chem       Date:  2019-07-04       Impact factor: 3.641

5.  1-(Fluoroalkylidene)-1,1-bisphosphonic acids are potent and selective inhibitors of the enzymatic activity of Toxoplasma gondii farnesyl pyrophosphate synthase.

Authors:  Sergio H Szajnman; Valeria S Rosso; Leena Malayil; Alyssa Smith; Silvia N J Moreno; Roberto Docampo; Juan B Rodriguez
Journal:  Org Biomol Chem       Date:  2012-01-03       Impact factor: 3.876

6.  In Vitro and In Vivo Activities of Sulfur-Containing Linear Bisphosphonates against Apicomplexan Parasites.

Authors:  Sergio H Szajnman; Tamila Galaka; Zhu-Hong Li; Catherine Li; Nathan M Howell; María N Chao; Boris Striepen; Vasant Muralidharan; Silvia N J Moreno; Juan B Rodriguez
Journal:  Antimicrob Agents Chemother       Date:  2017-01-24       Impact factor: 5.191

7.  Design, synthesis, calorimetry, and crystallographic analysis of 2-alkylaminoethyl-1,1-bisphosphonates as inhibitors of Trypanosoma cruzi farnesyl diphosphate synthase.

Authors:  Srinivas Aripirala; Sergio H Szajnman; Jean Jakoncic; Juan B Rodriguez; Roberto Docampo; Sandra B Gabelli; L Mario Amzel
Journal:  J Med Chem       Date:  2012-07-05       Impact factor: 7.446

8.  Radical reaction of sodium hypophosphite with terminal alkynes: synthesis of 1,1-bis-H-phosphinates.

Authors:  Sonia Gouault-Bironneau; Sylvine Deprèle; Amber Sutor; Jean-Luc Montchamp
Journal:  Org Lett       Date:  2005-12-22       Impact factor: 6.005

9.  Design, synthesis and biological evaluation of sulfur-containing 1,1-bisphosphonic acids as antiparasitic agents.

Authors:  Marion Recher; Alejandro P Barboza; Zhu-Hong Li; Melina Galizzi; Mariana Ferrer-Casal; Sergio H Szajnman; Roberto Docampo; Silvia N J Moreno; Juan B Rodriguez
Journal:  Eur J Med Chem       Date:  2012-12-20       Impact factor: 6.514

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

Authors:  Sergio H Szajnman; Guadalupe E García Liñares; Zhu-Hong Li; Cuiying Jiang; Melina Galizzi; Esteban J Bontempi; Marcela Ferella; Silvia N J Moreno; Roberto Docampo; Juan B Rodriguez
Journal:  Bioorg Med Chem       Date:  2007-12-10       Impact factor: 3.641

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