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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
*Corresponding author for this work
  • Georgia State University
    ,
  • Swiss Tropical and Public Health Institute
    ,
  • Ohio State University
Scholary Output:
Contribution to journal
Article
Peer-review

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.

Publication Information

Output type

Scholary Output:
Contribution to journal
Article
Peer-review

Original language

English (US)

Pages from-to (Number of pages)

Pages 552-557 (6 pages)

Journal (Volume, Issue Number)

European Journal of Medicinal Chemistry (Volume 42, Issue 4)

Publication milestones

  • Published - 04/2007

Publication status

Published - 04/2007

ISSN

0223-5234

Publication IDs

  • Scopus: 34047175303
  • PubMed: 17178177

Publication metrics

Metrics

Scopus
citations
Fractional count
1
Fractional count
0.11
Fractional count
8
Fractional count
0.89
Fractional count
1
Fractional count
1
SciVal
citations
52
SciVal
FWCI
1.91
SciVal
Author count
9
SciVal
Paper percentile
89

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Captures
38
Citation count
61

Funding Details

This work was supported by an award from the Bill and Melinda Gates Foundation and NIH grant GM61587. The technical assistance with the in vivo experiments by Guy Riccio (Swiss Tropical Institute) is greatly appreciated.
FundersFunding number
NIH
-
NIGMS
R01GM061587
BMGF
-