title: Effective bisquaternary reactivators of tabun-inhibited AChE.
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.
authors.affiliation: Department of Toxicology, Faculty of Military Health Sciences, Hradec Kralove, Czech Republic. kucakam@seznam.cz
authors.forename: Kamil
authors.initials: K
authors.lastname: Kuca
authors.forename: Jiri
authors.initials: J
authors.lastname: Cabal
authors.forename: Kamil
authors.initials: K
authors.lastname: Musilek
authors.forename: Daniel
authors.initials: D
authors.lastname: Jun
authors.forename: Jiri
authors.initials: J
authors.lastname: Bajgar
mesh_terms: D000110:Acetylcholinesterase / Q000737:chemistry / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000187:drug effects / Q000201:enzymology; D002073:Butanes / Q000737:chemistry / Q000494:pharmacology; D002800:Cholinesterase Inhibitors / Q000633:toxicity*; D002801:Cholinesterase Reactivators / Q000138:chemical synthesis / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005260:Female; D066298:In Vitro Techniques; D007700:Kinetics; D010755:Organophosphates / Q000633:toxicity*; D010091:Oximes / Q000138:chemical synthesis / Q000494:pharmacology*; D011726:Pyridinium Compounds; D011743:Pyrimidines / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
chemical_list: C515196:1,4-bis(4-hydroxyiminomethylpyridinium)butane dibromide; D002073:Butanes; D002800:Cholinesterase Inhibitors; D002801:Cholinesterase Reactivators; D010755:Organophosphates; D010091:Oximes; D011726:Pyridinium Compounds; D011743:Pyrimidines; D000110:Acetylcholinesterase; C009374:tabun