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Benzimidazole-based dual dipeptidyl peptidase-4 and xanthine oxidase inhibitors
dc.creator | Tomović, Katarina | |
dc.creator | Ilić, Budimir S. | |
dc.creator | Smelcerović, Zaklina | |
dc.creator | Miljković, Marija | |
dc.creator | Yancheva, Denitsa | |
dc.creator | Kojić, Milan | |
dc.creator | Mavrova, Anelia Ts | |
dc.creator | Kocić, Gordana | |
dc.creator | Smelcerović, Andrija | |
dc.date.accessioned | 2022-11-15T15:16:24Z | |
dc.date.available | 2022-11-15T15:16:24Z | |
dc.date.issued | 2020 | |
dc.identifier.issn | 0009-2797 | |
dc.identifier.uri | https://imagine.imgge.bg.ac.rs/handle/123456789/1376 | |
dc.description.abstract | Multiple-targeting compounds might reduce complex polypharmacy of multifactorial diseases, such as diabetes, and contribute to the greater therapeutic success. Targeting reactive oxygen species-producing enzymes, as xanthine oxidase (XO), might suppress progression of diabetes-associated vascular complications. In this study a small series of benzimidazole derivatives (1-9) was evaluated for inhibitory activity against dipeptidyl peptidase-4 (DPP-4) and XO. One 1,3-disubstituted-benzimidazole-2-imine (5) and 1,3-thiazolo [3,2-a] benzimidazolone derivative (8) were shown as effective dual DPP-4 and XO inhibitors, with IC50 values lower than 200 mu M, and predicted binding modes with both target enzymes. Both selected dual inhibitors (compounds 5 and 8) did not show cytotoxicity to a greater extent on Caco-2 cells even at concentration of 250 mu M. These structures represent new non-purine scaffolds bearing two therapeutic functionalities, being DPP-4 and XO inhibitors, more favorable in comparison to DPP-4 inhibitors with DPP-4 as a single target due to pleiotropic effects of XO inhibition. | en |
dc.publisher | Elsevier Ireland Ltd, Clare | |
dc.relation | Faculty of Medicine of the University of Nis [4] | |
dc.relation | L'Oreal Foundation | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172044/RS// | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/171025/RS// | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/173019/RS// | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Technological Development (TD or TR)/31060/RS// | |
dc.rights | restrictedAccess | |
dc.source | Chemico-Biological Interactions | |
dc.subject | Xanthine oxidase | en |
dc.subject | Molecular dynamics | en |
dc.subject | Dual inhibition | en |
dc.subject | Dipeptidyl peptidase-4 | en |
dc.subject | Cytotoxicity | en |
dc.subject | Benzimidazole | en |
dc.title | Benzimidazole-based dual dipeptidyl peptidase-4 and xanthine oxidase inhibitors | en |
dc.type | article | |
dc.rights.license | ARR | |
dc.citation.other | 315() | |
dc.citation.rank | M21 | |
dc.citation.volume | 315 | |
dc.identifier.doi | 10.1016/j.cbi.2019.108873 | |
dc.identifier.pmid | 31669219 | |
dc.identifier.scopus | 2-s2.0-85074070795 | |
dc.identifier.wos | 000514572800013 | |
dc.type.version | publishedVersion |
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