Synthesis and chemiluminescent high throughput screening for inhibition of acetylcholinesterase activity by imidazo[2,1-b]thiazole derivatives

Eur J Med Chem. 2005 Dec;40(12):1331-4. doi: 10.1016/j.ejmech.2005.05.010. Epub 2005 Aug 29.

Abstract

The synthesis of a new series of imidazo[2,1-b]thiazole derivatives is described. They were tested as acetylcholinesterase inhibitors by means of a chemiluminescent method suitable for high throughput screening. The compounds without quaternization had no appreciable inhibitory potency probably because they are poorly soluble in water. The corresponding quaternized compounds were good inhibitors with activity related to the spacer employed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholinesterase / drug effects*
  • Acetylcholinesterase / metabolism
  • Drug Evaluation, Preclinical
  • Imidazoles / chemical synthesis*
  • Imidazoles / chemistry
  • Imidazoles / pharmacology*
  • Luminescent Measurements / methods*
  • Molecular Structure
  • Sensitivity and Specificity
  • Structure-Activity Relationship
  • Thiazoles / chemical synthesis*
  • Thiazoles / chemistry
  • Thiazoles / pharmacology*

Substances

  • Imidazoles
  • Thiazoles
  • Acetylcholinesterase