quercetin-3-o-glucopyranoside and taxifolin

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.

Topics: Adenosine; Antitrichomonal Agents; Flavonoids; High-Throughput Screening Assays; N-Glycosyl Hydrolases; Quercetin; Small Molecule Libraries; Stereoisomerism; Trichomonas vaginalis