Design and synthesis of new bis-pyridinium oxime reactivators for acetylcholinesterase inhibited by organophosphorous nerve agents

Tae-Hyuk Kim; Kamil Kuca; Daniel Jun; Young-Sik Jung

doi:10.1016/j.bmcl.2005.03.060

Design and synthesis of new bis-pyridinium oxime reactivators for acetylcholinesterase inhibited by organophosphorous nerve agents

Bioorg Med Chem Lett. 2005 Jun 2;15(11):2914-7. doi: 10.1016/j.bmcl.2005.03.060. Epub 2005 Apr 21.

Authors

Tae-Hyuk Kim¹, Kamil Kuca, Daniel Jun, Young-Sik Jung

Affiliation

¹ Medicinal Science Division, Korea Research Institute of Chemical Technology, Yusong, Taejon.

PMID: 15911280
DOI: 10.1016/j.bmcl.2005.03.060

Abstract

New bis-pyridinium oxime reactivators connected with a CH(2)CH(2)OCH(2)CH(2) linker between two pyridinium rings were designed and synthesized. In the test of their potency to reactivate AChE inhibited by cyclosarin, the bis-pyridinium oxime 6b achieved reactivation potency higher than 10% at the lower concentration 10(-4)M.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Acetylcholinesterase / drug effects
Acetylcholinesterase / metabolism*
Cholinesterase Reactivators / chemical synthesis*
Cholinesterase Reactivators / pharmacology
Organophosphates / pharmacology*
Pyridinium Compounds / chemical synthesis*
Pyridinium Compounds / pharmacology*

Substances

Cholinesterase Reactivators
Organophosphates
Pyridinium Compounds
Acetylcholinesterase