AdoHcy hydrolase of Trichomonas vaginalis: Studies of the effects of 5 '-modified adenosine analogues and related 6-N-cyclopropyl derivatives

作者：Dornbush Padraick J; Vazquez Anaya Guillermo; Shokar Ajit; Benson Saoly; Rapp Magdalena; Wnuk Stanislaw F; Wrischnik Lisa A; Land Kirkwood M^*

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(24): 7466-7468.

DOI：10.1016/j.bmcl.2010.10.014

• Trichomonas vaginalis
• AdoHcy Hydrolase
• 5 '-Modified adenosine analogue
• 6-N-Cylcopropyl derivative

Trypanosoma brucei and Trichomonas vaginalis are both parasitic protozoans that are known to share many similar biochemical pathways. Aristeromycin, as well as 5 '-iodovinyl and 5 '-oxime analogues of adenosine, are potent inhibitors of AdoHcy hydrolase in T. brucei, an enzyme that catalyses the hydrolysis of AdoHcy to adenosine and L-homocysteine. To help determine the role of this enzyme in T. vaginalis, we have tested a library of 5 '-modified adenosine derivatives, including 5 '-deoxy-5 '-( iodomethylene)-adenosine and related 6-N-cyclopropyl analogues. Our results indicate that these inhibitors are effective at inhibiting the growth of T. vaginalis, by as much as 95%.

• 出版日期2010-12-15