Literature DB >> 16092078

Effective bisquaternary reactivators of tabun-inhibited AChE.

Kamil Kuca1, Jiri Cabal, Kamil Musilek, Daniel Jun, Jiri Bajgar.   

Abstract

Two cholinesterase reactivators (K074 and K075) were synthesized and their reactivation efficacy against tabun-inhibited acetylcholinesterase of the rat brain was tested in vitro. Comparing this efficacy showed that commonly used oximes (pralidoxim, obidoxime and HI-6) were practically without reactivation potency. On the other hand, oximes K074, K075 and trimedoxime were satisfactorily effective. Moreover, K-oximes reactivated tabun-inhibited AChE at lower concentration (10(-4) and 10(-3) m) in comparison with trimedoxime (10(-3) and 10(-2) m). Thus, K-oximes can be considered as the most effective reactivators of tabun-inhibited AChE at present. Copyright (c) 2005 John Wiley & Sons, Ltd.

Entities:  

Mesh:

Substances:

Year:  2005        PMID: 16092078     DOI: 10.1002/jat.1084

Source DB:  PubMed          Journal:  J Appl Toxicol        ISSN: 0260-437X            Impact factor:   3.446


  8 in total

1.  The present approaches to the development of prophylactic and therapeutic antidotes against nerve agents.

Authors:  Jiří Kassa; Jiří Bajgar; Kamil Kuča; Kamil Musílek; Jana Karasová
Journal:  Interdiscip Toxicol       Date:  2008-06

2.  Targeted synthesis of 1-(4-hydroxyiminomethylpyridinium)-3-pyridiniumpropane dibromide--a new nerve agent reactivator.

Authors:  Kamil Kuca; Kamil Musilek; Martin Paar; Daniel Jun; Petr Stodulka; Martina Hrabinova; Jan Marek
Journal:  Molecules       Date:  2007-08-20       Impact factor: 4.411

3.  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

4.  In vitro reactivation potency of acetylcholinesterase reactivators--K074 and K075--to reactivate tabun-inhibited human brain cholinesterases.

Authors:  Kamil Kuca; Jiri Cabal; Daniel Jun; Kamil Musilek
Journal:  Neurotox Res       Date:  2007-02       Impact factor: 3.911

5.  A newly developed oxime K203 is the most effective reactivator of tabun-inhibited acetylcholinesterase.

Authors:  Kamil Kuca; Kamil Musilek; Daniel Jun; Jana Zdarova-Karasova; Eugenie Nepovimova; Ondrej Soukup; Martina Hrabinova; John Mikler; Tanos C C Franca; Elaine F F Da Cunha; Alexandre A De Castro; Martin Valis; Teodorico C Ramalho
Journal:  BMC Pharmacol Toxicol       Date:  2018-02-21       Impact factor: 2.483

6.  Toxic Injury to Muscle Tissue of Rats Following Acute Oximes Exposure.

Authors:  Vesna Jaćević; Eugenie Nepovimova; Kamil Kuča
Journal:  Sci Rep       Date:  2019-02-06       Impact factor: 4.379

7.  Novel Group of AChE Reactivators-Synthesis, In Vitro Reactivation and Molecular Docking Study.

Authors:  David Malinak; Eugenie Nepovimova; Daniel Jun; Kamil Musilek; Kamil Kuca
Journal:  Molecules       Date:  2018-09-07       Impact factor: 4.411

8.  Acute Toxic Injuries of Rat's Visceral Tissues Induced by Different Oximes.

Authors:  Vesna Jaćević; Eugenie Nepovimova; Kamil Kuča
Journal:  Sci Rep       Date:  2019-11-11       Impact factor: 4.379

  8 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.