Synthesis and Research of Reactivation of Phosphorylated Cholinesterase by Quaternary Pyridinium-aldoxime Salts
نویسنده
چکیده
The interaction of pyridine-4(-3,-2)aldoxime has been studied whit 3-bromo-N,N,N-trialkyl-2oxo(-hydroxyimino)-1-propanaminium bromide. The structure of all synthesized compounds was determined by elemental analysis as well as by physical and chemical methods. All synthesized compounds were tested for reactivation of phosphorylated acetylcholinesterase. Using fragments of the molecules (an oxime group, 3-bromoN,N,N-trimethyl(or triethyl)ammonium [(or N-methylmorpholinium)-2-oxo(or 2-hydroxyimino)]propan bromides), a new series of pyridinium-aldoxime salt (cholinesterase reactivator) was obtained.
منابع مشابه
Synthesis and disinfection effect of the pyridine-4-aldoxime based salts.
A set of new quaternary ammonium compounds based on pyridine-4-aldoxime was synthesized, characterized with analytical data (NMR, EA, HPLC, MS) and tested for in vitro antimicrobial activity (antibacterial, antifungal) and cytotoxicity. Quaternary pyridinium-4-aldoxime salts with length of alkyl side chain from C8 to C20 and belonging to the group of cationic surfactants were investigated in th...
متن کاملStructure-activity approach in the reactivation of tabun-phosphorylated human acetylcholinesterase with bispyridinium para-aldoximes.
We investigated interactions of bispyridinium para-aldoximes N,N'-(propano)bis(4-hydroxyiminomethyl) pyridinium bromide (TMB-4), N,N'-(ethano)bis(4-hydroxyiminomethyl)pyridinium methanosulphonate (DMB-4), and N,N'-(methano)bis(4-hydroxyiminomethyl)pyridinium chloride (MMB-4) with human erythrocyte acetylcholinesterase phosphorylated by tabun. We analysed aldoxime conformations to determine the ...
متن کاملSubstituted monoquaternary oximes as reactivators of cyclosarin--and chlorpyrifos--inhibited acetylcholinesterase.
This paper describes an in vitro study of three potential acetylcholinesterase (AChE; EC 3.1.1.7) reactivators derived from a monoquaternary reactivator pralidoxime. Compounds used were pyridinium-2-aldoxime-4-carbamoyl-N-methyl iodide (TO231), pyridinium-2-aldoxime-4-ethoxycarbonyl-N-methyl iodide (TO237), and pyridinium-2-aldoxime-5-ethoxycarbonyl-N-methyl iodide (TO238). Pralidoxime and obid...
متن کاملCholinesterase reactivation in vivo with a novel bis-oxime optimized by computer-aided design.
Recently, several bis-pyridiniumaldoximes linked by a variable-length alkylene chain were rationally designed in our laboratories as cholinesterase reactivators. Extensive in vitro tests of these oximes with acetylcholinesterase inhibited by two different organophosphate agents, echothiophate and diisopropylfluorophosphate, revealed one compound with particularly good reactivation kinetics and ...
متن کاملOxime reactivation of diethylphosphoryl human serum cholinesterase.
Reactivation of diethyl p-nitrophenyl phosphate inhibited human serum cholinesterase by pyridine-Z-aldoxime methiodide and isonitrosoacetophenone has been investigated as a function of reactivator concentration, pH, and temperature in boric acid-borax buffer and in salt solution. Constants shown were the dissociation constants of the diethylphosphoryl cholinesterase reactivator complex for the ...
متن کامل