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AdoHcy hydrolase of Trichomonas vaginalis: studies of the effects of 5'-modified adenosine analogues and related 6-N-cyclopropyl derivatives.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Dec 15; Vol. 20 (24), pp. 7466-8. Date of Electronic Publication: 2010 Oct 31. - Publication Year :
- 2010
-
Abstract
- Trypanosoma brucei and Trichomonas vaginalis are both parasitic protozoans that are known to share many similar biochemical pathways. Aristeromycin, as well as 5'-iodovinyl and 5'-oxime analogues of adenosine, are potent inhibitors of AdoHcy hydrolase in T. brucei, an enzyme that catalyses the hydrolysis of AdoHcy to adenosine and L-homocysteine. To help determine the role of this enzyme in T. vaginalis, we have tested a library of 5'-modified adenosine derivatives, including 5'-deoxy-5'-(iodomethylene)-adenosine and related 6-N-cyclopropyl analogues. Our results indicate that these inhibitors are effective at inhibiting the growth of T. vaginalis, by as much as 95%.<br /> (Copyright © 2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- Adenosine chemical synthesis
Adenosine chemistry
Adenosine pharmacology
Adenosylhomocysteinase metabolism
Amino Acid Sequence
Antiprotozoal Agents chemical synthesis
Antiprotozoal Agents pharmacology
Molecular Sequence Data
Sequence Alignment
Structure-Activity Relationship
Adenosine analogs & derivatives
Adenosylhomocysteinase antagonists & inhibitors
Antiprotozoal Agents chemistry
Cyclopropanes chemistry
Trichomonas vaginalis enzymology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 20
- Issue :
- 24
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21044841
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.10.014