Triazoxins: Novel nucleosides with anti-Giardia activity
[Display omitted] 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 cul...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2020-06, Vol.30 (12), p.127175-127175, Article 127175 |
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Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | [Display omitted]
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. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2020.127175 |