MMSL 2018, 87(88):116

NOVEL BISQUATERNARY HETEROAROMATIC COMPOUNDS AS POTENTIAL REACTIVATORS OF HUMAN BUTYRYLCHOLINESTERASEMeeting abstracts

David Malinak1,2, Eugenie Nepovimova1, Marketa Neugebauerova1, Miroslava Hozova2, Vendula Hepnarova ORCID...3, Daniel Jun ORCID...3, Rafael Dolezal ORCID...1,2, Kamil Musilek ORCID...1,2, Kamil Kuca ORCID...1
1 University of Hradec Kralove, Faculty of Science, Department of Chemistry, Rokitanskeho 62, 500 03 Hradec Kralove, Czech Republic
2 University Hospital Hradec Kralove, Biomedical Research Centre, Sokolska 581, 500 05 Hradec Kralove, Czech Republic
3 University of Defence, Faculty of Military Health Sciences, Department of Toxicology and Military Pharmacy, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic

Human butyrylcholinesterase (hBChE) is well-known stoichiometric scavenger in case of organophosphorus (OP) intoxication. However, its major limitation lies in binding of only one OP moiety per hBChE molecule and thus necessity of its very high dosage prior or post intoxication. This issue might be resolved by use of hBChE reactivators that could cleave irreversibly bound OP moiety from the enzyme active site and restore its scavenging function. This concept has been called pseudo-catalytic scavenger. Within our contribution, we would like to present bisquaternary heteroaromatic compounds that are butyrylcholinesterase reactivators and might act as potential pseudo-catalytic bioscavengers. Recently, we have prepared and evaluated over 20 novel compounds that displayed better hBChE reactivation activity than clinically used reactivators.

Published: September 2, 2018  Show citation

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Malinak, D., Nepovimova, E., Neugebauerova, M., Hozova, M., Hepnarova, V., Jun, D., ... Kuca, K. (2018). NOVEL BISQUATERNARY HETEROAROMATIC COMPOUNDS AS POTENTIAL REACTIVATORS OF HUMAN BUTYRYLCHOLINESTERASE. MMSL87(Suppl.1), 116
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