Affiliation: Faculty of Military Health Sciences
Country: Czech Republic
Musilek K, Holas O, Kuca K, Jun D, Dohnal V, Dolezal M. Synthesis of a novel series of non-symmetrical bispyridinium compounds bearing a xylene linker and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase. J Enzyme Inhib Med Chem. 2007;22:425-32 pubmed
..Seven compounds were promising against paraoxon-inhibited AChE. Two compounds were found to be more potent against tabun-inhibited AChE than obidoxime at a concentration applicable in vivo. ..
Musilek K, Dolezal M, Gunn Moore F, Kuca K. Design, evaluation and structure-activity relationship studies of the AChE reactivators against organophosphorus pesticides. Med Res Rev. 2011;31:548-75 pubmed publisher
..Some of these are highlighted for their further testing of OPP exposure and, additionally, the main structure-activity relationship of AChE reactivators against OPP is discussed. ..
Musilek K, Holas O, Kuca K, Jun D, Dohnal V, Opletalova V, et al
. Synthesis of monooxime-monocarbamoyl bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against tabun- and paraoxon-inhibited acetylcholinesterase. J Enzyme Inhib Med Chem. 2008;23:70-6 pubmed
..The best results were obtained for bisquaternary substances with at least one oxime group in position four. ..
Musilek K, Kucera J, Jun D, Dohnal V, Opletalova V, Kuca K. Monoquaternary pyridinium salts with modified side chain-synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase. Bioorg Med Chem. 2008;16:8218-23 pubmed publisher
..However, extensive differences were found by a SAR study for various side chains on the non-oxime part of the reactivator molecule. ..