IRREVERSIBLE INHIBITOR OF SARCOPLASMIC RETICULUM Ca-ADENOSINE TRIPHOSPHATASE Russian patent published in 2002 - IPC

FIELD: biochemistry, organic chemistry. SUBSTANCE: invention relates to the use of derivatives of 1,2-benzisothiazole-3-one of the general formula given in the invention where R¹ means lower alkyl or phenyl and R² is H or NO₂ which are used as irreversible inhibitor of Ca²⁺-adenosine triphosphatase of sarcoplasmic reticulum (SERCA). Derivatives of 1,2-benzisothiaxole- -3-one of the general formula given in the invention exhibit the more expressed irreversible effect on SERCA as compared with its analog, i. e. 7-chloro-4-nitrobenz-2,1,3- oxadiazole (NBD-Cl). NBD-Cl under close conditions inhibits enzyme irreversibly also but its effect eliciting in concentration 0.75 mM is compared with effect of 6-nitro-2-phenyl-1,2- -benzisothiazole-3-one in concentration 0.15 mM. EFFECT: valuable biochemical properties of inhibitor. 1 tbl, 1 dwg