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Literature DB >> 16759117

DNA binding affinity of bisguanidine and bis(2-aminoimidazoline) derivatives with in vivo antitrypanosomal activity.

Christophe Dardonville¹, Michael P Barrett, Reto Brun, Marcel Kaiser, Farial Tanious, W David Wilson.

Abstract

A new antitrypanosomal hit compound that cures an acute (STIB 900) mouse model of Trypanosoma brucei rhodesiense trypanosomiasis is described. This bis(2-aminoimidazolinium) dicationic compound proved to be an excellent DNA minor groove binder, suggesting a possible mechanism for its trypanocidal activity. From these studies, the 4,4'-diaminodiphenylamine skeleton emerged as a good scaffold for antitrypanosomal drugs.

Entities: Chemical Disease Species

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Year: 2006 PMID： 16759117 DOI： 10.1021/jm060295c

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

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Cited

14 in total

1. Functional and structural analysis of AT-specific minor groove binders that disrupt DNA-protein interactions and cause disintegration of the Trypanosoma brucei kinetoplast.

Authors: Cinthia R Millan; Francisco J Acosta-Reyes; Laura Lagartera; Godwin U Ebiloma; Leandro Lemgruber; J Jonathan Nué Martínez; Núria Saperas; Christophe Dardonville; Harry P de Koning; J Lourdes Campos
Journal: Nucleic Acids Res Date: 2017-08-21 Impact factor: 16.971

2. Antiprotozoal activity of 1-phenethyl-4-aminopiperidine derivatives.

Authors: Christophe Dardonville; Cristina Fernández-Fernández; Sarah-Louise Gibbons; Nadine Jagerovic; Lidia Nieto; Gary Ryan; Marcel Kaiser; Reto Brun
Journal: Antimicrob Agents Chemother Date: 2009-06-29 Impact factor: 5.191

3. Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.

Authors: Andriy Buchynskyy; J Robert Gillespie; Matthew A Hulverson; Joshua McQueen; Sharon A Creason; Ranae M Ranade; Nicole A Duster; Michael H Gelb; Frederick S Buckner
Journal: Bioorg Med Chem Date: 2016-11-12 Impact factor: 3.641

4. Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis.

Authors: Hari Babu Tatipaka; J Robert Gillespie; Arnab K Chatterjee; Neil R Norcross; Matthew A Hulverson; Ranae M Ranade; Pendem Nagendar; Sharon A Creason; Joshua McQueen; Nicole A Duster; Advait Nagle; Frantisek Supek; Valentina Molteni; Tanja Wenzler; Reto Brun; Richard Glynne; Frederick S Buckner; Michael H Gelb
Journal: J Med Chem Date: 2014-01-15 Impact factor: 7.446

5. Rapid Determination of Ionization Constants (pK a) by UV Spectroscopy Using 96-Well Microtiter Plates.

Authors: Carlos H Ríos Martínez; Christophe Dardonville
Journal: ACS Med Chem Lett Date: 2012-11-20 Impact factor: 4.345

6. A new nonpolar N-hydroxy imidazoline lead compound with improved activity in a murine model of late-stage Trypanosoma brucei brucei infection is not cross-resistant with diamidines.

Authors: Carlos H Ríos Martínez; Florence Miller; Kayathiri Ganeshamoorthy; Fabienne Glacial; Marcel Kaiser; Harry P de Koning; Anthonius A Eze; Laura Lagartera; Tomás Herraiz; Christophe Dardonville
Journal: Antimicrob Agents Chemother Date: 2014-11-24 Impact factor: 5.191

DNA binding affinity of bisguanidine and bis(2-aminoimidazoline) derivatives with in vivo antitrypanosomal activity.

1. Functional and structural analysis of AT-specific minor groove binders that disrupt DNA-protein interactions and cause disintegration of the Trypanosoma brucei kinetoplast.

2. Antiprotozoal activity of 1-phenethyl-4-aminopiperidine derivatives.

3. Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.

4. Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis.

5. Rapid Determination of Ionization Constants (pK a) by UV Spectroscopy Using 96-Well Microtiter Plates.

6. A new nonpolar N-hydroxy imidazoline lead compound with improved activity in a murine model of late-stage Trypanosoma brucei brucei infection is not cross-resistant with diamidines.

7. Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis.

8. Understanding the DNA binding of novel non-symmetrical guanidinium/2-aminoimidazolinium derivatives.

9. Crystal structure of a trypanocidal 4,4'-bis(imidazolinylamino)diphenylamine bound to DNA.

10. Neglected disease - african sleeping sickness: recent synthetic and modeling advances.