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ISSN 2410-7751 (Print)
ISSN 2410-776X (Online)

"Biotechnologia Acta" v. 6, no. 2, 2013
Р. 80-84, Bibliography 14, Russian.
Universal Decimal classification: 577.152.311/547.8/548.73


E. A. Shesterenko, I. I. Romanovska, O. V. Sevastyanov, E. A. Semenishina
V. I. Pavlovsky, S. A. Andronati

Bogatsky’s Physico-Chemical Institute of National Academy of Sciences of Ukraine, Odesa

The synthesis of new series of 7-bromo-5-aryl-1,2-dihydro-3H-1,4-benzdiazepine-2-one derivatives, containing in the tree position phthalimidoacyl and hexylacyl fragments was accomplished. The structure of new compounds was proved by mass-spectrometry and PMRspectroscopy methods. For the first time, hydrolysis of the earlier synthesized 3-hydroxy-7-bromo-5-aryl-1,2-dihydro-3H-1,4-benzdiazepine-2-one esters, potential anxiolytic and hypnotic means, catalyzed by carboxyl esterase in composition of pig liver microsomal fraction was studied. The quantitative inhibition of pig liver microsomal fraction esterase activity in the presence of carboxyl esterase selective inhibitor di-(pnitrophenyl)-phosphate was shown. The nonlinear dependence both of hydrolysis degree with acyl moiety length in 3-acyloxy-7-bromo-5-aryl-1,2-dihydro-3H-1,4-benzdiazepine-2-ones and decreased substrate transformation degree after substituent introduction in the first position of molecule was established. For the derivatives with phthalimidoacyl and hexylacyl-mo ie ties in the molecule 3 position it was shown, that increasing of CH2-groups number in this substituents and incorporation of chlorine atom in o-position of phenyl ring bring to increasing of hydrolysis degree.

Key words: 3-hydroxy-1,4-benzdiazepine-2-one esters, carboxyl esterase, microsomal fraction.

© Palladin Institute of Biochemistry of National Academy of Sciences of Ukraine, 2013