S-Adenosylhomocysteine hydrolase of the protozoan parasite Trichomonas vaginalis: Potent inhibitory activity of 9-(2-deoxy-2-fluoro-β,d-arabinofuranosyl)adenine

Bioorganic & Medicinal Chemistry Letters
2012.0

Abstract

In the present study, we carried out a structure-activity analysis in Trichomonas vaginalis of a series of adenosine and uridine analogues. The most potent compounds were found to be 2' and 3' modified adenosine analogues some of which are potent inhibitors of S-adenosylhomocysteine hydrolase. The 9-(2-deoxy-2-fluoro-β,D-arabinofuranosyl)adenine compound was more potent than metronidazole, a current FDA approved and commonly prescribed drug for treatment of trichomoniasis. Its IC(50) was 0.09 μM compared to 0.72 μM for metronidazole.

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