Trichomonas vaginalis is the causative agent of trichomoniasis, a common sexually-transmitted disease in humans. Approximately 5% of cases of trichomoniasis are resistant to treatment with the commonly prescribed metronidazole.  The search for alternative new therapies for both nitroimidazole susceptible and resistant cases is imperative.  The various purine and pyrimidine nucleoside analogues modified at C2', C3' and C5' of the ribose ring and at position C2 and C6 of the adenine ring were tested against T. vaginalis in vitro. The most potent compounds were found to be 2'-modified adenosine derivatives especially ones having arabino configuration. Thus, 2'-deoxy-2'-fluoroadenosine, 9-(�,D-arabinofuranosyl)adenine,  9-(2-deoxy-2-fluoro-�,D-arabinofuranosyl)adenine , and 9-(2-chloro-2-deoxy-�,D-arabinofuranosyl)adenine    inhibit T. vaginalis 100% at 100 �M level. These compounds have an IC50 of 2.94 �M, 3.6 �M, 0.09 �M, and 5.93 �M, respectively (Metronidazole's IC50 value for the same strain is 0.72 �M).

Inhibition of adenosylhomocysteine hydrolase of <i>Trichomonas vaginalis</i> with 9-(2-deoxy-2-fluoro-β,D-arabinofuranosyl)adenine

243rd National Meeting (2012)

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Inhibition of adenosylhomocysteine hydrolase of Trichomonas vaginalis with 9-(2-deoxy-2-fluoro-β,D-arabinofuranosyl)adenine