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

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 IC50 was 0.09μM compared to 0.72μM for metronidazole.