In-vitro Evaluation of Bis-pyridinium Oximes Connected by Xylene Linkers as Reactivators of DFP-inhibited Electric EEL Acetylcholinesterase

  • Jyotiranjan Acharya Process Technology Development Division, Defence Research & Development Establishment, Gwalior
  • Hitendra N Karade Process Technology Development Division, Defence Research & Development Establishment, Gwalior
  • G Raviraju Process Technology Development Division, Defence Research & Development Establishment, Gwalior
  • Sanatan Ghosh Process Technology Development Division, Defence Research & Development Establishment, Gwalior
  • Arvind Kumar Gupta Process Technology Development Division, Defence Research & Development Establishment, Gwalior
Keywords: Bis-pyridinium oximes, Reactivators, 2-PAM, DFP, organophosphorus pesticides, nerve agents, acetylcholinesterase, obidoxime

Abstract

Bis-pyridinium oximes connected by xylene linkers were synthesised and their in-vitro reactivation efficacy was evaluated for DFP inhibited AChE. The reactivation efficacy data were compared with those of 2-PAM and obidoxime. However, it was observed that none of these oximes were able to surpass the reactivation efficacy of 2-PAM and obidoxime in reactivating DFP inhibited AChE. 2-PAM and obidoxime respectively exhibited
52 per cent and 43 per cent reactivation of DFP inhibited AChE, where as the synthesised oximes 3a, 3d, and 3f showed 37 per cent, 30 per cent, and 31 per cent reactivation, respectively within 10 min at 10-3 M.

Author Biographies

Jyotiranjan Acharya, Process Technology Development Division, Defence Research & Development Establishment, Gwalior
Dr Jyotiranjan Acharya received his MSc (Organic Chemistry) and PhD (Medicinal Chemistry) from Jiwaji University, Gwalior, India, in 1999 and 2008, respectively. Currently, he is a Scientist in Defence Research & Development Establishment, Gwalior, India. His area of interest includes : Development of antidotes against anticholinesterase agents.
Hitendra N Karade, Process Technology Development Division, Defence Research & Development Establishment, Gwalior
Dr Hitendra N. Karade did his MSc (Organic Chemistry) from Amaravati University, Amaravati, India in 2002 and PhD in Chemistry from Jiwaji University, Gwalior, India in 2008. Currently, he is a Scientist in Defence Research & Development Establishment, Gwalior, India. His area of interest includes : Development of antidotes against anticholinesterase agents as well as synthesis of small bioactive molecules.
G Raviraju, Process Technology Development Division, Defence Research & Development Establishment, Gwalior
Mr G. Raviraju received his MSc in physical chemistry from Andhra University, Vishakapatnam, India in 2009. Currently he is Scientist in Defence Research & Development Establishment, Gwalior, India. His area of interest includes : Development of antidotes against anticholinesterase agents
Sanatan Ghosh, Process Technology Development Division, Defence Research & Development Establishment, Gwalior
Mr Sanatan Ghosh received his MSc degree in chemistry from The University of Burdwan, Burdwan, West Bengal in 2013. Currently he is Senior Technical Assistant in Defence Research & Development Establishment (DRDE) Gwalior, India. His area of interest includes : Design synthesis and evaluation of antidotes against nerve agent poisoning
Arvind Kumar Gupta, Process Technology Development Division, Defence Research & Development Establishment, Gwalior
Dr Aravind Kumar Gupta received his MSc in chemistry and PhD from Jiwaji University, Gwalior, India in 1987 and 2003, respectively. Currently he is Scientist in Defence Research & Development Establishment, Gwalior, India. His area of interest includes : Synthesis, characterisation and analysis of chemical warfare agents and their antidotes.
Published
2016-10-07
How to Cite
AcharyaJ., KaradeH., RavirajuG., GhoshS., & GuptaA. (2016). In-vitro Evaluation of Bis-pyridinium Oximes Connected by Xylene Linkers as Reactivators of DFP-inhibited Electric EEL Acetylcholinesterase. Defence Life Science Journal, 1(2), 162-166. https://doi.org/10.14429/dlsj.1.10736
Section
Research Article