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• W2999077049 abstract "P-glycoprotein (P-gp) is an ATP-dependent efflux pump that has a marked impact on the absorption, distribution, and excretion of therapeutic drugs. As P-gp inhibition can result in drug-drug interactions and altered drug bioavailability, identifying molecular properties that are linked to inhibition is of great interest in drug development. In this study, we combined chemical synthesis, in vitro testing, quantitative structure-activity relationship analysis, and docking studies to investigate the role of hydrogen bond (H-bond) donor/acceptor properties in transporter-ligand interaction. In a previous work, it has been shown that propafenone analogs with a 4-hydroxy-4-piperidine moiety exhibit a generally 10-fold higher P-gp inhibitory activity than expected based on their lipophilicity. Here, we specifically expanded the data set by introducing substituents at position 4 of the 4-phenylpiperidine moiety to assess the importance of H-bond donor/acceptor features in this region. The results suggest that indeed an H-bond acceptor, such as hydroxy and methoxy, increases the affinity by forming a H-bond with Tyr310." @default.
• W2999077049 created "2020-01-23" @default.
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• W2999077049 date "2020-01-09" @default.
• W2999077049 modified "2023-10-14" @default.
• W2999077049 title "Propafenone analogue with additional H‐bond acceptor group shows increased inhibitory activity on P‐glycoprotein" @default.
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• W2999077049 doi "https://doi.org/10.1002/ardp.201900269" @default.
• W2999077049 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/31917466" @default.
• W2999077049 hasPublicationYear "2020" @default.
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