Adenosylhomocysteine hydrolase of the protozoan parasite Trichomonas vaginalis: Potent inhibitory activity of 9-(2-deoxy-2-fluoro-β, D-arabinofuranosyl) adenine
ORCID
Kirkwood M. Land: 0000-0001-5951-9630
Document Type
Article
Publication Title
Bioorganic and Medicinal Chemistry Letters
Department
Biological Sciences
ISSN
0960-894X
Volume
22
Issue
12
DOI
10.1016/j.bmcl.2012.03.087
First Page
4203
Last Page
4205
Publication Date
6-15-2012
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 0.09 μM compared to 0.72 μM for metronidazole.
Recommended Citation
Shokar, A.,
Au, A.,
Hwan An, S.,
Tong, E.,
Garza, G.,
Zayas, J.,
Wnuk, S. F.,
&
Land, K. M.
(2012).
Adenosylhomocysteine hydrolase of the protozoan parasite Trichomonas vaginalis: Potent inhibitory activity of 9-(2-deoxy-2-fluoro-β, D-arabinofuranosyl) adenine.
Bioorganic and Medicinal Chemistry Letters, 22(12), 4203–4205.
DOI: 10.1016/j.bmcl.2012.03.087
https://scholarlycommons.pacific.edu/cop-facarticles/777
