RUS  ENG
Full version
JOURNALS // Uspekhi Khimii // Archive

Usp. Khim., 1991 Volume 60, Issue 8, Pages 1744–1776 (Mi rcr958)

This article is cited in 12 papers

S-alkynyl esters of phosphorus thioacids as inhibitors of cholinesterases and as promising physiologically active compounds

A. P. Brestkin, L. A. Vikhreva, N. N. Godovikov, Yu. G. Zhukovskii, M. I. Kabachnik, S. N. Moralev, V. I. Rosengart, O. E. Sherstobitov

A. N. Nesmeyanov Institute of Organoelement Compounds, USSR Academy of Sciences, Moscow

Abstract: Data are given in the review on the anticholinesterase activity of 58 specially synthesised esters of phosphorus thioacids containing an acetylenic bond in the thioester group. It was established that compounds containing an acetylenic group in the β and especially in the α position of the thioester residue display an inhibitory action many times greater than that of their saturated analogues. A phosphorylated enzyme is formed by the reaction of the acetylenic organophosphorus inhibitors (OPIs) with the enzymes as in the case of reaction with the saturated analogues. It was shown that the acetylenic organophosphorus inhibitors possess high biological activity both for mammals and for arthropods. On replacing the phosphoryl oxygen (P=O) by sulphur (P=S) the toxicity of the acetylenic organophosphorus inhibitors for mammals was sharply reduced but was little changed for arthropods. This raises the possibility of obtaining highly selective insecto-acaricides. The mechanism of the antienzymic action of the acetylenic OPIs and the mechanism of detoxication of diethyl S-hexynyl dithiophosphate are considered. The bibliography includes 44 references.

UDC: 577.1

DOI: 10.1070/RC1991v060n08ABEH001117


 English version:
Russian Chemical Reviews, 1991, 60:8, 885–902

Bibliographic databases:


© Steklov Math. Inst. of RAS, 2024