Literature DB >> 18341256

Synthesis of monooxime-monocarbamoyl bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against tabun- and paraoxon-inhibited acetylcholinesterase.

Kamil Musilek1, Ondrej Holas, Kamil Kuca, Daniel Jun, Vlastimil Dohnal, Veronika Opletalova, Martin Dolezal.   

Abstract

Six AChE monooxime-monocarbamoyl reactivators with an (E)-but-2-ene linker were synthesized using modification of currently known synthetic pathways. Their potency to reactivate AChE inhibited by the nerve agent tabun and insecticide paraoxon was tested in vitro. The reactivation efficacies of pralidoxime, HI-6, obidoxime, K048, K075 and the newly prepared reactivators were compared. According to the results obtained, one reactivator seems to be promising against tabun-inhibited AChE and two reactivators against paraoxon-inhibited AChE. The best results were obtained for bisquaternary substances with at least one oxime group in position four.

Entities:  

Mesh:

Substances:

Year:  2008        PMID: 18341256     DOI: 10.1080/14756360701383981

Source DB:  PubMed          Journal:  J Enzyme Inhib Med Chem        ISSN: 1475-6366            Impact factor:   5.051


  5 in total

1.  New series of monoquaternary pyridinium oximes: Synthesis and reactivation potency for paraoxon-inhibited electric eel and recombinant human acetylcholinesterase.

Authors:  Sandip B Bharate; Lilu Guo; Tony E Reeves; Douglas M Cerasoli; Charles M Thompson
Journal:  Bioorg Med Chem Lett       Date:  2009-07-10       Impact factor: 2.823

2.  Effect of several new and currently available oxime cholinesterase reactivators on tabun-intoxicated rats.

Authors:  Jana Zdarova Karasova; Jiri Kassa; Young-Sik Jung; Kamil Musilek; Miroslav Pohanka; Kamil Kuca
Journal:  Int J Mol Sci       Date:  2008-11-14       Impact factor: 6.208

3.  Effect of seven newly synthesized and currently available oxime cholinesterase reactivators on cyclosarin-intoxicated rats.

Authors:  Jana Zdarova Karasova; Jiri Kassa; Kamil Musilek; Miroslav Pohanka; Ladislav Novotny; Kamil Kuca
Journal:  Int J Mol Sci       Date:  2009-07-07       Impact factor: 6.208

Review 4.  Trends in the Recent Patent Literature on Cholinesterase Reactivators (2016-2019).

Authors:  Alexandre A de Castro; Letícia C Assis; Flávia V Soares; Kamil Kuca; Daniel A Polisel; Elaine F F da Cunha; Teodorico C Ramalho
Journal:  Biomolecules       Date:  2020-03-12

5.  Understanding the Interaction Modes and Reactivity of Trimedoxime toward MmAChE Inhibited by Nerve Agents: Theoretical and Experimental Aspects.

Authors:  Alexandre A de Castro; Daniel A Polisel; Bruna T L Pereira; Elaine F F da Cunha; Kamil Kuca; Eugenie Nepovimova; Teodorico C Ramalho
Journal:  Int J Mol Sci       Date:  2020-09-05       Impact factor: 5.923

  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.