KINETIC FEATURES OF HYDROLYSIS OF 3-HYDROXY-1,4- BENZОDIAZEPINE-2-ONE ESTERS WITH A HELP OF PIG LIVER MICROSOMAL FRACTION
The kinetic features of new 3-hydroxy-1,4-benzоdiazepine-2-ones esters hydrolysis with a help of pig liver microsomal fraction, isolated using the low-speed sedimentation method in the presence of Ca2+-ions, were studied. The total inhibition of porcine microsomal fraction esterase activity be carbo...
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| Format: | Article |
| Language: | English |
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Odessa I. I. Mechnikov National University
2014-12-01
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| Series: | Vìsnik Odesʹkogo Nacìonalʹnogo Unìversitetu: Hìmìâ |
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| Online Access: | http://heraldchem.onu.edu.ua/article/view/32008 |
| Summary: | The kinetic features of new 3-hydroxy-1,4-benzоdiazepine-2-ones esters hydrolysis with a help of pig liver microsomal fraction, isolated using the low-speed sedimentation method in the presence of Ca2+-ions, were studied. The total inhibition of porcine microsomal fraction esterase activity be carboxylesterase selective inhibitor – bis-(p-nitrophenyl) phosphate was shown,which is an evidence of such an enzyme involvement in studied substrates hydrolysis. The nonlinearity of maximal rate, Vmax, and Michaelis constant, KM, of 3-acyloxy-5-phenyl-1,2-dihydro-3H-1,4-benzodiazepin-2-ones hydrolysis dependence from acyl moiety length in the 3 position, and also Vmax lowering due to substitutes introduction in the first position of molecule, was established. |
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| ISSN: | 2304-0947 2414-5963 |