Literature DB >> 11206471

Polyamines with N-(3-phenylpropyl) substituents are effective competitive inhibitors of trypanothione reductase and trypanocidal agents.

Z Li1, M W Fennie, B Ganem, M T Hancock, M Kobaslija, D Rattendi, C J Bacchi, M C O'Sullivan.   

Abstract

Several N-(3-phenylpropyl)-substituted spermidine and spermine derivatives were prepared and found to be potent competitive inhibitors of Trypanosoma cruzi trypanothione reductase (seven compounds with Ki values < 5 microM are described). The most effective inhibitor studied was compound 12 with a Ki value of 0.151 microM. Six of the compounds described are also effective trypanocides with IC50 values < 1 microM.

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Year:  2001        PMID: 11206471     DOI: 10.1016/s0960-894x(00)00643-0

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


  11 in total

Review 1.  Parasite-specific trypanothione reductase as a drug target molecule.

Authors:  R Luise Krauth-Siegel; Oliver Inhoff
Journal:  Parasitol Res       Date:  2003-04-23       Impact factor: 2.289

2.  Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity.

Authors:  Georgina A Holloway; William N Charman; Alan H Fairlamb; Reto Brun; Marcel Kaiser; Edmund Kostewicz; Patrizia M Novello; John P Parisot; John Richardson; Ian P Street; Keith G Watson; Jonathan B Baell
Journal:  Antimicrob Agents Chemother       Date:  2009-04-13       Impact factor: 5.191

3.  A neural networks study of quinone compounds with trypanocidal activity.

Authors:  Fábio Alberto de Molfetta; Wagner Fernando Delfino Angelotti; Roseli Aparecida Francelin Romero; Carlos Alberto Montanari; Albérico Borges Ferreira da Silva
Journal:  J Mol Model       Date:  2008-07-16       Impact factor: 1.810

4.  Discovery of novel alkylated (bis)urea and (bis)thiourea polyamine analogues with potent antimalarial activities.

Authors:  Bianca K Verlinden; Jandeli Niemand; Janette Snyman; Shiv K Sharma; Ross J Beattie; Patrick M Woster; Lyn-Marie Birkholtz
Journal:  J Med Chem       Date:  2011-09-14       Impact factor: 7.446

5.  Novel alkylpolyamine analogues that possess both antitrypanosomal and antimicrosporidial activity.

Authors:  Y Zou; Z Wu; N Sirisoma; P M Woster; R A Casero; L M Weiss; D Rattendi; S Lane; C J Bacchi
Journal:  Bioorg Med Chem Lett       Date:  2001-06-18       Impact factor: 2.823

6.  Trypanothione reductase: a viable chemotherapeutic target for antitrypanosomal and antileishmanial drug design.

Authors:  M Omar F Khan
Journal:  Drug Target Insights       Date:  2007-06-19

7.  Exploiting members of the BAHD acyltransferase family to synthesize multiple hydroxycinnamate and benzoate conjugates in yeast.

Authors:  Aymerick Eudes; Maxence Mouille; David S Robinson; Veronica T Benites; George Wang; Lucien Roux; Yi-Lin Tsai; Edward E K Baidoo; Tsan-Yu Chiu; Joshua L Heazlewood; Henrik V Scheller; Aindrila Mukhopadhyay; Jay D Keasling; Samuel Deutsch; Dominique Loqué
Journal:  Microb Cell Fact       Date:  2016-11-21       Impact factor: 5.328

8.  Investigation of trypanothione reductase as a drug target in Trypanosoma brucei.

Authors:  Daniel Spinks; Emma J Shanks; Laura A T Cleghorn; Stuart McElroy; Deuan Jones; Daniel James; Alan H Fairlamb; Julie A Frearson; Paul G Wyatt; Ian H Gilbert
Journal:  ChemMedChem       Date:  2009-12       Impact factor: 3.466

9.  Improved tricyclic inhibitors of trypanothione reductase by screening and chemical synthesis.

Authors:  John L Richardson; Isabelle R E Nett; Deuan C Jones; Mohamed H Abdille; Ian H Gilbert; Alan H Fairlamb
Journal:  ChemMedChem       Date:  2009-08       Impact factor: 3.466

Review 10.  Experimental and Clinical Treatment of Chagas Disease: A Review.

Authors:  Policarpo Ademar Sales Junior; Israel Molina; Silvane Maria Fonseca Murta; Adrián Sánchez-Montalvá; Fernando Salvador; Rodrigo Corrêa-Oliveira; Cláudia Martins Carneiro
Journal:  Am J Trop Med Hyg       Date:  2017-10-10       Impact factor: 2.345

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