title: Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes.
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.
authors.affiliation: Department of Chemistry and Center for Biotechnology and Drug Design, Georgia State University, University Plaza, Atlanta, GA 30303-3083, USA.
authors.forename: Jose L
authors.initials: JL
authors.lastname: Gonzalez
authors.forename: Chad E
authors.initials: CE
authors.lastname: Stephens
authors.forename: Tanja
authors.initials: T
authors.lastname: Wenzler
authors.forename: Reto
authors.initials: R
authors.lastname: Brun
authors.forename: Farial A
authors.initials: FA
authors.lastname: Tanious
authors.forename: W David
authors.initials: WD
authors.lastname: Wilson
authors.forename: Todd
authors.initials: T
authors.lastname: Barszcz
authors.forename: Karl A
authors.initials: KA
authors.lastname: Werbovetz
authors.forename: David W
authors.initials: DW
authors.lastname: Boykin
mesh_terms: D000818:Animals; D000977:Antiparasitic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004195:Disease Models, Animal; D006146:Guanidines / Q000737:chemistry; D007891:Leishmania / Q000187:drug effects*; D051379:Mice; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010961:Plasmodium / Q000187:drug effects*; D013876:Thiophenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014345:Trypanosoma / Q000187:drug effects*
chemical_list: D000977:Antiparasitic Agents; D006146:Guanidines; D013876:Thiophenes