Triazoxins: Novel nucleosides with anti-Giardia activity

Praveen K. Pogula, Atasi De Chatterjee, Miguel Chi, Harrison W. VanKoten, Siddhartha Das, Steven E. Patterson

Research output: Contribution to journalArticlepeer-review

Abstract

Novel nucleoside analogues named “triazoxins” were synthesized. Of these, two analogues were found to be highly effective against Giardia lamblia, an intestinal parasite and a major cause of waterborne infection, worldwide. While compound 7 reduced the growth of trophozoites in culture (IC50, ~5 μM), compound 21 blocked the in vitro cyst production (IC50 ~5 μM). Compound 21 was also effective against trophozoites (IC50, ~36 μM). A third analogue (compound 8) was effective against both trophozoites (IC50, ~36 μM) and cysts (IC50, ~20 μM) although at higher concentration. Thus triazoxin analogues are unique and exhibit morphology (i.e., trohozoites or cysts) -specific effects against Giardia.

Original languageEnglish (US)
Article number127175
JournalBioorganic and Medicinal Chemistry Letters
Volume30
Issue number12
DOIs
StatePublished - Jun 15 2020

Bibliographical note

Funding Information:
We thank the Center for Drug Design, and NIH- NIAID grant 1R21AI138061 for funding this project. Cellular experiments were carried out in the Border Biomedical Research Center (BBRC) core Facility at the University of Texas at El Paso supported by a grant ( G12MD0075592 ) from the NIMHD (NIH). ADC and SD were supported partly by a grant ( R01AI095667 ) from the NIH ( NIAID ). MC was supported by NIH-RISE Grant 5R25GM069621 .

Funding Information:
We thank the Center for Drug Design, and NIH-NIAID grant 1R21AI138061 for funding this project. Cellular experiments were carried out in the Border Biomedical Research Center (BBRC) core Facility at the University of Texas at El Paso supported by a grant (G12MD0075592) from the NIMHD (NIH). ADC and SD were supported partly by a grant (R01AI095667) from the NIH (NIAID). MC was supported by NIH-RISE Grant 5R25GM069621.

Publisher Copyright:
© 2020 Elsevier Ltd

Keywords

  • Anti-giardiasis
  • Cyst
  • Giardia
  • Phosphonoxin
  • Triazoxin
  • Trophozoite

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