173352-21-1Relevant articles and documents
The giardicidal activity of lobendazole, fabomotizole, tenatoprazole and ipriflavone: A ligand-based virtual screening and in vitro study
Pérez-Villanueva, Jaime,Yépez-Mulia, Lilián,Rodríguez-Villar, Karen,Cortés-Benítez, Francisco,Palacios-Espinosa, Juan Francisco,Soria-Arteche, Olivia
, (2021)
A ligand-based virtual screening study to search for giardicidal compounds on a 6551 ChEMBL drugs database was carried out using molecular similarity. Three fingerprints implemented in MayaChemTools with different design and validated by ROC curves, were used. Twelve compounds were retrieved from this screening, from which, four representative compounds were selected to carry out biological assays. Whereas two compounds were commercially available, the additional two compounds were synthesized during the development of this work. The biological assays revealed that the compounds possess in vitro activity against five strains of Giardia intestinalis, each with different susceptibility/resistance rates to metronidazole, albendazole and nitazoxanide. Particularly, tenatoprazole showed the best effect against the WB and IMSS strains. Furthermore, fabomotizole, tenatoprazole and ipriflavone showed a higher activity against resistant strains than the reference drugs: metronidazole, albendazole and nitazoxanide.
2-mercaptobenzimidazole derivatives possessing pharmacological activity
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, (2008/06/13)
2-mercaptobenzimidazole derivatives of the general formula wherein: N=0,2,3; R-hydrogen atom, aralkyls; R1-lower alkyls, alkenyls, dialkylamino, a saturated amine monocyclic residue which may contain an additional heteroatom; R2and R3/sup