Literature DB >> 17178177

Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes.

Jose L Gonzalez1, Chad E Stephens, Tanja Wenzler, Reto Brun, Farial A Tanious, W David Wilson, Todd Barszcz, Karl A Werbovetz, David W Boykin.   

Abstract

A series of bis-2,5-[4-guanidinophenyl]thiophenes were prepared in a five step process starting from 2,5-bis[trimethylstannyl]thiophene. The compounds were evaluated in vitro against Trypanosoma brucei rhodesiense (T. b. r.), Plasmodium falciparum (P. f.), Leshmania donovani (L. d.) and Trypanasoma cruzi (T. c.), and in vivo against T. b. r. Certain compounds show promising in vitro activity against T. b. r. and P. f. and have superior in vivo activity against T. b. r. to that of pentamidine and furamidine.

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Year:  2006        PMID: 17178177     DOI: 10.1016/j.ejmech.2006.11.006

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  10 in total

1.  Characterization of a melamino nitroheterocycle as a potential lead for the treatment of human african trypanosomiasis.

Authors:  Federica Giordani; Annamaria Buschini; Alessandro Baliani; Marcel Kaiser; Reto Brun; Michael P Barrett; Claudia Pellacani; Paola Poli; Ian H Gilbert
Journal:  Antimicrob Agents Chemother       Date:  2014-07-14       Impact factor: 5.191

2.  In vitro efficacy of dicationic compounds and mefloquine enantiomers against Echinococcus multilocularis metacestodes.

Authors:  Britta Stadelmann; Tatiana Küster; Sabrina Scholl; Fabienne Barna; Christian Kropf; Jennifer Keiser; David W Boykin; Chad E Stephens; Andrew Hemphill
Journal:  Antimicrob Agents Chemother       Date:  2011-07-18       Impact factor: 5.191

3.  Discovery of novel polyamine analogs with anti-protozoal activity by computer guided drug repositioning.

Authors:  Lucas N Alberca; María L Sbaraglini; Darío Balcazar; Laura Fraccaroli; Carolina Carrillo; Andrea Medeiros; Diego Benitez; Marcelo Comini; Alan Talevi
Journal:  J Comput Aided Mol Des       Date:  2016-02-18       Impact factor: 3.686

4.  Pentamidine analogs as inhibitors of [(3)H]MK-801 and [(3)H]ifenprodil binding to rat brain NMDA receptors.

Authors:  Michael L Berger; Dorota Maciejewska; Jean Jacques Vanden Eynde; Madhusoodanan Mottamal; Jerzy Żabiński; Paweł Kaźmierczak; Mateusz Rezler; Ivana Jarak; Ivo Piantanida; Grace Karminski-Zamola; Annie Mayence; Patrick Rebernik; Arvind Kumar; Mohamed A Ismail; David W Boykin; Tien L Huang
Journal:  Bioorg Med Chem       Date:  2015-06-14       Impact factor: 3.641

Review 5.  State of the art in African trypanosome drug discovery.

Authors:  Robert T Jacobs; Bakela Nare; Margaret A Phillips
Journal:  Curr Top Med Chem       Date:  2011       Impact factor: 3.295

6.  Novel linear triaryl guanidines, N-substituted guanidines and potential prodrugs as antiprotozoal agents.

Authors:  Reem K Arafa; Mohamed A Ismail; Manoj Munde; W David Wilson; Tanja Wenzler; Reto Brun; David W Boykin
Journal:  Eur J Med Chem       Date:  2008-02-29       Impact factor: 6.514

7.  Antileishmanial Mechanism of Diamidines Involves Targeting Kinetoplasts.

Authors:  Gyongseon Yang; Gahee Choi; Joo Hwan No
Journal:  Antimicrob Agents Chemother       Date:  2016-10-21       Impact factor: 5.191

8.  Simple colorimetric trypanothione reductase-based assay for high-throughput screening of drugs against Leishmania intracellular amastigotes.

Authors:  Erika van den Bogaart; Gerard J Schoone; Paul England; Dorien Faber; Kristina M Orrling; Jean-Claude Dujardin; Shyam Sundar; Henk D F H Schallig; Emily R Adams
Journal:  Antimicrob Agents Chemother       Date:  2013-11-04       Impact factor: 5.191

9.  Synthesis and anticancer activity of di(3-thienyl)methanol and di(3-thienyl)methane.

Authors:  Nagendra Kumar Kaushik; Hong Seon Kim; Young June Chae; Young Nam Lee; Gi-Chung Kwon; Eun Ha Choi; In Tae Kim
Journal:  Molecules       Date:  2012-09-27       Impact factor: 4.411

10.  Synthesis and biological evaluation of N-cyanoalkyl-, N-aminoalkyl-, and N-guanidinoalkyl-substituted 4-aminoquinoline derivatives as potent, selective, brain permeable antitrypanosomal agents.

Authors:  Irene Sola; Albert Artigas; Martin C Taylor; F Javier Pérez-Areales; Elisabet Viayna; M Victòria Clos; Belén Pérez; Colin W Wright; John M Kelly; Diego Muñoz-Torrero
Journal:  Bioorg Med Chem       Date:  2016-08-22       Impact factor: 3.641

  10 in total

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