AldoHcy Hydrolase of Trichomonas vaginalis: Studies of the effects of 5'-deoxy-5'-(iodomethylene) adenosine and related 6-N-cyclopropyladenosine analogues on in vitro culture

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

20

Issue

24

DOI

10.1016/j.bmcl.2010.10.014

First Page

7466

Last Page

7468

Publication Date

12-1-2010

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%

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