Pharmaceutical Chemistry Journal

, Volume 29, Issue 2, pp 87–88 | Cite as

Features of the anticholinesterase effect of oxaphopholanol derivatives

  • R. S. Garaev
Molecular Biological Problems in Drug Design and the Mechanism of Drug Action


The anticholinesterase effect in vitro of 14 derivatives of oxaphosfolanol (2-P-2-oxo(thioxo)-3.5.5-trimethyl-1,2-oxophosfolan-3-ol) on brain homogenate, blood serum, and purified enzyme preparations of acetylcholinesterase and butyrylcholinesterase (BuChE) was studied. Some representatives of these compounds exhibited a weak anticholinesterase effect in a concentration of 10 mliter/liter, The cholinesterase (ChE) of the brain homogenate inhibited by 50% by the thiophosphoryl analogue of the ethyl ether of oxaphosfolanol was not reactivated by dipyroxime. In experiments involving blood serum and BuChE, the degree of inhibition of the enzyme by oxaphosfolanol ethers was correlated with the hydrophobicity of the compounds. The possibility was postulated of inhibiting ChE by oxaphosfolanol derivatives as a result of hydrophobic reactions without phosphorylation of the esterase center of the enzyme.


Ether Ethyl Organic Chemistry Blood Serum Cholinesterase 
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Copyright information

© Plenum Publishing Corporation 1995

Authors and Affiliations

  • R. S. Garaev
    • 1
  1. 1.Kazan Medical InstituteKazanRussia

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