Bi_2020_Bioorg.Chem_100_103902

Reference

Title : Design, synthesis and evaluation of novel nonquaternary and 3 non-oxime reactivators for acetylcholinesterase inhibited by organophosphates - Bi_2020_Bioorg.Chem_100_103902
Author(s) : Bi H , Ouyang Q , Wei Z , Zheng Z
Ref : Bioorg Chem , 100 :103902 , 2020
Abstract :

A new series of novel nonquaternary conjugates and non-oxime reactivators for reactivation of both nerve agents and pesticides inhibited hAChE were described in this paper. Conjugates with piperazine linked to the substituted salicylaldoxime emerged as efficient reactivators for VX inhibited hAChE. The in vitro reactivation experiment showed that some of them were equal or more efficient reactivators for pesticides inhibited hAChE than obidoxime. It was also found that some non-oxime derivatives of Mannich phenols displayed obvious reactivation potency for VX, sarin and pesticides inhibited hAChE even in very low concentration. It has been proved that introduction of peripheral site ligands with widespread aromatic system and amide substitutions could increase binding affinity for inhibited hAChE in most cases, which contribute to the reactivation efficiency.

PubMedSearch : Bi_2020_Bioorg.Chem_100_103902
PubMedID: 32388435

Related information

Citations formats

Bi H, Ouyang Q, Wei Z, Zheng Z (2020)
Design, synthesis and evaluation of novel nonquaternary and 3 non-oxime reactivators for acetylcholinesterase inhibited by organophosphates
Bioorg Chem 100 :103902

Bi H, Ouyang Q, Wei Z, Zheng Z (2020)
Bioorg Chem 100 :103902