Gonzalez JL1, Stephens CE, Wenzler T, Brun R, Tanious FA, Wilson WD, Barszcz T, Werbovetz KA, Boykin DW.
Eur J Med Chem. 2007 Apr;42(4):552-7. Epub 2006 Nov 22.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.