TY - JOUR
T1 - Triazoxins
T2 - Novel nucleosides with anti-Giardia activity
AU - Pogula, Praveen K.
AU - De Chatterjee, Atasi
AU - Chi, Miguel
AU - VanKoten, Harrison W.
AU - Das, Siddhartha
AU - Patterson, Steven E.
N1 - Publisher Copyright:
© 2020 Elsevier Ltd
PY - 2020/6/15
Y1 - 2020/6/15
N2 - 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.
AB - 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.
KW - Anti-giardiasis
KW - Cyst
KW - Giardia
KW - Phosphonoxin
KW - Triazoxin
KW - Trophozoite
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U2 - 10.1016/j.bmcl.2020.127175
DO - 10.1016/j.bmcl.2020.127175
M3 - Article
C2 - 32327222
AN - SCOPUS:85083390739
SN - 0960-894X
VL - 30
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 12
M1 - 127175
ER -