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

  • K. Musílek EMAIL logo , L. Lipka , V. Račáková , K. Kuča , D. Jun , V. Dohnal und M. Doležal
Veröffentlicht/Copyright: 1. Februar 2006
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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.

[1] Bajgar, J., Adv. Clin. Chem. 38, 151 (2004). http://dx.doi.org/10.1016/S0065-2423(04)38006-610.1016/S0065-2423(04)38006-6Suche in Google Scholar

[2] Marrs, T. C., Pharmacol. Ther. 58, 51 (1993). http://dx.doi.org/10.1016/0163-7258(93)90066-M10.1016/0163-7258(93)90066-MSuche in Google Scholar

[3] Patočka, J., Kuča, K., and Jun, D., Acta Med. (Hradec Králové) 47, 215 (2004). 10.14712/18059694.2018.95Suche in Google Scholar

[4] Kuča, K., Bielavský, J., Cabal, J., and Kassa, J., Bioorg. Med. Chem. Lett. 13, 3545 (2003). http://dx.doi.org/10.1016/S0960-894X(03)00751-010.1016/S0960-894X(03)00751-0Suche in Google Scholar

[5] Kassa, J., J. Toxicol., Clin. Toxicol. 40, 803 (2002). http://dx.doi.org/10.1081/CLT-12001584010.1081/CLT-120015840Suche in Google Scholar

[6] Kuča, K., Bielavský, J., Cabal, J., and Bielavská, M., Tetrahedron Lett. 44, 3123 (2003). http://dx.doi.org/10.1016/S0040-4039(03)00538-010.1016/S0040-4039(03)00538-0Suche in Google Scholar

[7] Wilson, I. B., Ginsburg, S., and Meilisch, E. K., J. Am. Chem. Soc. 77, 4286 (1955). http://dx.doi.org/10.1021/ja01621a03510.1021/ja01621a035Suche in Google Scholar

[8] Poziomek, E. J., Hackley, B. E., and Steinberg, G. M., J. Org. Chem. 23, 714 (1958). http://dx.doi.org/10.1021/jo01099a01910.1021/jo01099a019Suche in Google Scholar

[9] Krejčová, G. and Kassa, J., Toxicology 185, 129 (2003). http://dx.doi.org/10.1016/S0300-483X(02)00599-110.1016/S0300-483X(02)00599-1Suche in Google Scholar

[10] Rousseaux, C. G. and Gua, A. K., Can. J. Physiol. Pharmacol. 67, 1183 (1989). Suche in Google Scholar

[11] Kassa, J., Cabal, J., Bajgar, J., and Szinicz, L., ASA Newslett. 97-4, 16 (1997). Suche in Google Scholar

[12] Krejčová, G., Ševelová, L., and Kuča, K., Zprav. Voj. Farm. 14, 5 (2004). Suche in Google Scholar

[13] Hampl, F., Mazač, J., Liška, F., Šrogl, J., Kábrt, L., and Suchánek, M., Collect. Czech. Chem. Commun. 60, 883 (1995). http://dx.doi.org/10.1135/cccc1995088310.1135/cccc19950883Suche in Google Scholar

[14] Kuča, K., Cabal, J., Patočka, J., and Kassa, J., Lett. Org. Chem. 1, 84 (2004). http://dx.doi.org/10.2174/157017804348876110.2174/1570178043488761Suche in Google Scholar

[15] Pang, Y. P., Kollmeyer, T. M., Hong, F., Lee, J. C., Hammond, P. I., Haugabouk, S. P., and Brimijoin, S., Chem. Biol. 10, 491 (2003). http://dx.doi.org/10.1016/S1074-5521(03)00126-110.1016/S1074-5521(03)00126-1Suche in Google Scholar

[16] Kuča, K. and Kassa, J., J. Enzyme Inhib. Med. Chem. 18, 529 (2003). http://dx.doi.org/10.1080/1475636031000160555210.1080/14756360310001605552Suche in Google Scholar PubMed

[17] Kuča, K. and Patočka, J., J. Enzyme Inhib. Med. Chem. 19, 39 (2004). http://dx.doi.org/10.1080/147563603100016385010.1080/1475636031000163850Suche in Google Scholar PubMed

[18] Kuča, K., Patočka, J., and Cabal, J., J. Appl. Biomed. 1, 207 (2003). Suche in Google Scholar

[19] Ginsburg, S. and Wilson, I. B., J. Am. Chem. Soc. 79, 481 (1957). http://dx.doi.org/10.1021/ja01559a06710.1021/ja01559a067Suche in Google Scholar

[20] Waysbort, D., Balderman, D., and Amitai, G., Org. Magn. Reson. 16, 7 (1981). http://dx.doi.org/10.1002/mrc.127016010310.1002/mrc.1270160103Suche in Google Scholar

[21] Sikder, A. K., Ghosh, A. K., and Jaiswal, D. K., J. Pharm. Sci. 82, 258 (1993). http://dx.doi.org/10.1002/jps.260082030810.1002/jps.2600820308Suche in Google Scholar PubMed

Published Online: 2006-2-1
Published in Print: 2006-2-1

© 2006 Institute of Chemistry, Slovak Academy of Sciences

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