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 journalArticlepeer-review

57 Scopus citations


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
Issue number4
StatePublished - Apr 2007
Externally publishedYes


  • Antiparasitic agents
  • Diguanidino thiophenes

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry


Dive into the research topics of 'Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes'. Together they form a unique fingerprint.

Cite this