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

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• 作者：Ajit Shokar^a ; Aaron Au^a ; Seung Hwan An^a ; Elsie Tong^b ; Gabriel Garza^b ; Jessica Zayas^c ; Stanislaw F. Wnuk^c ; Kirkwood M. Land^a ; ^{kland@pacific.edu}
• 关键词：Trichomonas vaginalis ; Anti-protozoal drug ; S-Adenosylhomocysteine hydrolase
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 June, 2012
• 卷：22
• 期：12
• 页码：4203-4205
• 文件大小：321 K

摘要

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鈥?and 3鈥?modified adenosine analogues some of which are potent inhibitors of S-adenosylhomocysteine hydrolase. The 9-(2-deoxy-2-fluoro-尾,d-arabinofuranosyl)adenine compound was more potent than metronidazole, a current FDA approved and commonly prescribed drug for treatment of trichomoniasis. Its IC₅₀ was 0.09 渭M compared to 0.72 渭M for metronidazole.