| Literature DB >> 26592812 |
Sierra Beck1, Samantha N Muellers1, Annie Laurie Benzie1, David W Parkin1, Brian J Stockman2.
Abstract
Nucleoside salvage pathway enzymes used by Trichomonas vaginalis are distinct from the pathway involved in activation of existing 5-nitroimidazole drugs. They thus represent excellent targets for developing novel, mechanism-based antitrichomonal agents. The purine-specific adenosine/guanosine preferring ribohydrolase (AGNH) was screened against the NIH Clinical Collection to assess its druggability. Eight compounds, including five flavonoids, were identified with IC50 values ⩽10 μM and confirmed in counter screens run in the presence of detergent. The inhibitors are structurally distinct from inhibitors of the pyrimidine-specific uridine ribohydrolase (UNH) thus indicating that AGNH is a distinct, druggable target from UNH.Entities:
Keywords: Flavonoids; NIH Clinical Compound Collection; NMR; Nucleoside ribohydrolase; Trichomonas vaginalis
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Year: 2015 PMID: 26592812 DOI: 10.1016/j.bmcl.2015.10.030
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823