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

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

Research output: Contribution to journalArticle

52 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)552-557
Number of pages6
JournalEuropean Journal of Medicinal Chemistry
Volume42
Issue number4
DOIs
StatePublished - Apr 1 2007
Externally publishedYes

Keywords

  • Antiparasitic agents
  • Diguanidino thiophenes

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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    Gonzalez, J. L., Stephens, C. E., Wenzler, T., Brun, R., Tanious, F. A., Wilson, W. D., Barszcz, T., Werbovetz, K. A., & Boykin, D. W. (2007). Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes. European Journal of Medicinal Chemistry, 42(4), 552-557. https://doi.org/10.1016/j.ejmech.2006.11.006