Alkyl 2-arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropionates as new effective and selective inhibitors of carboxylesterase / Boltneva N. P.,Makhaeva G. F.,Kovaleva N. V.,Lushchekina S. V.,Burgart Ya. V.,Shchegol'kov E. V.,Saloutin V. I.,Chupakhin O. N. // DOKLADY BIOCHEMISTRY AND BIOPHYSICS. - 2015. - V. 465, l. 1. - P. 381-385.

ISSN/EISSN:

1607-6729 / 1608-3091

Type:

Article

Abstract:

A series of alkyl 2-Arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropionates was synthesized and their inhibitory activity with respect to porcine liver carboxylesterase (CaE, EC 3.1.1.1), human erythrocyte acetylcholinesterase (AChE, EC 3.1.1.7), and horse serum butyrylcholinesterase (BChE, EC 3.1.1.8) was studied. The molecular docking method was used to study the binding mode of the compounds in the active site of CaE. It was found that compounds containing the trifluoromethyl group in the third position of carbonyl chain are highly effective and selective inhibitors of CaE with nanomolar IC50 values, which agrees well with the results of molecular docking.

Author keywords:

CRESYL SALIGENIN PHOSPHATE; BUTYRYLCHOLINESTERASE

DOI:

10.1134/S1607672915060101

Web of Science ID:

ISI:000367609900010

Соавторы в МНС:

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Другие поля

Поле	Значение
Month	NOV
Publisher	MAIK NAUKA/INTERPERIODICA/SPRINGER
Address	233 SPRING ST, NEW YORK, NY 10013-1578 USA
Language	English
EISSN	1608-3091
Keywords-Plus	CRESYL SALIGENIN PHOSPHATE; BUTYRYLCHOLINESTERASE
Research-Areas	Biochemistry \& Molecular Biology; Biophysics
Web-of-Science-Categories	Biochemistry \& Molecular Biology; Biophysics
Author-Email	boltneva@ipac.ac.ru
ResearcherID-Numbers	Makhaeva, Galina/A-9412-2014 Burgart, Yanina/T-8025-2017 Kovaleva, Nadezhda/F-8258-2017 Lushchekina, Sofya/F-8469-2010 Shchegol'kov, Evgenii/H-6790-2015
ORCID-Numbers	Burgart, Yanina/0000-0001-6061-2410 Lushchekina, Sofya/0000-0002-6922-020X Shchegol'kov, Evgenii/0000-0001-6611-2855
Funding-Acknowledgement	Dynasty Foundation
Funding-Text	In this study, we used the equipment of the Collective-Access Share Equipment of the Institute of Physiologically Active Compounds, Russian Academy of Sciences (agreement no. 14.621.21.0008, ID no. RFMEFI62114X0008). The work of S.V. Lushchekina was supported by a Dynasty Foundation scholarship.
Number-of-Cited-References	14
Usage-Count-Last-180-days	1
Usage-Count-Since-2013	8
Journal-ISO	Dokl. Biochem. Biophys.
Doc-Delivery-Number	DA2FE