ISSN print edition: 0366-6352 ISSN electronic edition: 1336-9075 Registr. No.: MK SR 9/7 Published monthly

New methods in synthesis of acetylcholinesterase reactivators and evaluation of their potency to reactivate cyclosarin-inhibited AChE

K. Musílek, L. Lipka, V. Račáková, K. Kuča, D. Jun, V. Dohnal, and M. Doležal

Department of Pharmaceutical Chemistry and Drug Control, Faculty of Pharmacy in Hradec Králové, Charles University in Prague, CZ-500 05 Hradec Králové, Czech Republic

E-mail: kucakam@pmfhk.cz

Received: 7 March 2005  Revised: 30 June 2005  Accepted: 7 July 2005

Abstract: Nine potential AChE reactivators were synthesized using modification of currently known synthetic pathways. Their potency to reactivate AChE inhibited by cyclosarin nerve agent was tested in vitro. According to the previous results, 1,4-bis(2-hydroxyiminomethylpyridinium)butane dibromide seems to be the most potent AChE reactivator. The reactivation potency of these compounds depends on structural factors such as presence of quaternary nitrogens, length of the linking chain between both pyridinium rings, and position of the oxime moiety at the pyridinium ring.

Full paper is available at www.springerlink.com.

DOI: 10.2478/s11696-006-0008-x

Chemical Papers 60 (1) 48–51 (2006)