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Literature DB >> 12760897

Mechanism of action of 4-phenoxyphenoxyethyl thiocyanate (WC-9) against Trypanosoma cruzi, the causative agent of Chagas' disease.

Julio A Urbina¹, Juan Luis Concepcion, Andrea Montalvetti, Juan B Rodriguez, Roberto Docampo.

Abstract

We investigated the molecular basis of the activity of 4-phenoxyphenoxyethyl thiocyanate (WC-9) against Trypanosoma cruzi, the etiological agent of Chagas' disease. We found that growth inhibition of T. cruzi epimastigotes induced by this compound was associated with a reduction in the content of the parasite's endogenous sterols due to a specific blockade of their de novo synthesis at the level of squalene synthase.

Entities: Chemical Disease Species

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Year: 2003 PMID： 12760897 PMCID： PMC155860 DOI： 10.1128/AAC.47.6.2047-2050.2003

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

22 in total

Review 1. Recent developments in the chemotherapy of Chagas disease.

Authors: R Docampo
Journal: Curr Pharm Des Date: 2001-08 Impact factor: 3.116

2. Squalene synthase as a chemotherapeutic target in Trypanosoma cruzi and Leishmania mexicana.

Authors: Julio A Urbina; Juan Luis Concepcion; Salomé Rangel; Gonzalo Visbal; Renee Lira
Journal: Mol Biochem Parasitol Date: 2002 Nov-Dec Impact factor: 1.759

3. Bisphosphonates are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase.

Authors: A Montalvetti; B N Bailey; M B Martin; G W Severin; E Oldfield; R Docampo
Journal: J Biol Chem Date: 2001-07-02 Impact factor: 5.157

4. Squalene synthase: steady-state, pre-steady-state, and isotope-trapping studies.

Authors: E S Radisky; C D Poulter
Journal: Biochemistry Date: 2000-02-22 Impact factor: 3.162

Review 5. Chemotherapy of Chagas disease.

Authors: Julio A Urbina
Journal: Curr Pharm Des Date: 2002 Impact factor: 3.116

Review 6. Specific treatment of Chagas disease: current status and new developments.

Authors: J A Urbina
Journal: Curr Opin Infect Dis Date: 2001-12 Impact factor: 4.915

7. Recombinant squalene synthase. A mechanism for the rearrangement of presqualene diphosphate to squalene.

Authors: Brian S J Blagg; Michael B Jarstfer; Daniel H Rogers; C Dale Poulter
Journal: J Am Chem Soc Date: 2002-07-31 Impact factor: 15.419

8. Recombinant squalene synthase. Synthesis of non-head-to-tail isoprenoids in the absence of NADPH.

Authors: Michael B Jarstfer; Dong-Lu Zhang; C Dale Poulter
Journal: J Am Chem Soc Date: 2002-07-31 Impact factor: 15.419

9. Antiproliferative effects and mechanism of action of SCH 56592 against Trypanosoma (Schizotrypanum) cruzi: in vitro and in vivo studies.

Authors: J A Urbina; G Payares; L M Contreras; A Liendo; C Sanoja; J Molina; M Piras; R Piras; N Perez; P Wincker; D Loebenberg
Journal: Antimicrob Agents Chemother Date: 1998-07 Impact factor: 5.191

10. Design, synthesis, and biological evaluation of aryloxyethyl thiocyanate derivatives against Trypanosoma cruzi.

Authors: Eleonora Elhalem; Brian N Bailey; Roberto Docampo; István Ujváry; Sergio H Szajnman; Juan B Rodriguez
Journal: J Med Chem Date: 2002-08-29 Impact factor: 7.446

14 in total

1. 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

2. 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

3. 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

4. Head-to-head prenyl tranferases: anti-infective drug targets.

Authors: Fu-Yang Lin; Yi-Liang Liu; Kai Li; Rong Cao; Wei Zhu; Jordan Axelson; Ran Pang; Eric Oldfield
Journal: J Med Chem Date: 2012-05-01 Impact factor: 7.446

5. Aryloxyethyl Thiocyanates Are Potent Growth Inhibitors of Trypanosoma cruzi and Toxoplasma gondii.

Authors: María N Chao; Carolina Exeni Matiuzzi; Melissa Storey; Catherine Li; Sergio H Szajnman; Roberto Docampo; Silvia N J Moreno; Juan B Rodriguez
Journal: ChemMedChem Date: 2015-04-27 Impact factor: 3.466

6. Design, synthesis and biological evaluation of WC-9 analogs as antiparasitic agents.

Authors: Pablo D Elicio; María N Chao; Melina Galizzi; Catherine Li; Sergio H Szajnman; Roberto Docampo; Silvia N J Moreno; Juan B Rodriguez
Journal: Eur J Med Chem Date: 2013-09-18 Impact factor: 6.514

7. 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

8. Fluorine-containing aryloxyethyl thiocyanate derivatives are potent inhibitors of Trypanosoma cruzi and Toxoplasma gondii proliferation.

Authors: Guadalupe García Liñares; Santiago Gismondi; Nicolás Osa Codesido; Silvia N J Moreno; Roberto Docampo; Juan B Rodriguez
Journal: Bioorg Med Chem Lett Date: 2007-07-13 Impact factor: 2.823

9. In vitro and in vivo activities of E5700 and ER-119884, two novel orally active squalene synthase inhibitors, against Trypanosoma cruzi.

Authors: Julio A Urbina; Juan Luis Concepcion; Aura Caldera; Gilberto Payares; Cristina Sanoja; Takeshi Otomo; Hironobu Hiyoshi
Journal: Antimicrob Agents Chemother Date: 2004-07 Impact factor: 5.191

10. Toxoplasma gondii relies on both host and parasite isoprenoids and can be rendered sensitive to atorvastatin.

Authors: Zhu-Hong Li; Srinivasan Ramakrishnan; Boris Striepen; Silvia N J Moreno
Journal: PLoS Pathog Date: 2013-10-17 Impact factor: 6.823