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

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

  • Eur J Med Chem. 2007 Apr;42(4):552-7. doi: 10.1016/j.ejmech.2006.11.006.
Jose L Gonzalez 1,  Chad E Stephens,  Tanja Wenzler,  Reto Brun,  Farial A Tanious,  W David Wilson,  Todd Barszcz,  Karl A Werbovetz,  David W Boykin
Affiliations

Affiliation

  • 1 Department of Chemistry and Center for Biotechnology and Drug Design, Georgia State University, University Plaza, Atlanta, GA 30303-3083, USA.
PMID: 17178177 DOI: 10.1016/j.ejmech.2006.11.006
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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