Selective Carboxylesterase Inhibitors for Improving Efficacy, Safety and Rational use of Ester-Containing Drugs

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Published: Jul 12, 2018
DOI: https://doi.org/10.18097/BMCRM00026
Keywords:
carboxylesterases prodrugs ester-containing drugs inhibitors polyfluoroalkyl-2-imino-1,3-dione scaffold

Main Article Content

N.P. Boltneva
Institute of Physiologically Active Compounds of the Russian Academy of Sciences, 1 Severny proezd, Moscow region, Chernogolovka, 142432 Russia
G.F. Makhaeva
Institute of Physiologically Active Compounds of the Russian Academy of Sciences, 1 Severny proezd, Moscow region, Chernogolovka, 142432 Russia
E.V. Shchegol’kov
Postovsky Institute of Organic Synthesis, Urals Branch of Russian Academy of Sciences, 22/20, S. Kovalevskoy/Akademicheskaya str., Yekaterinburg, 620990 Russia
Ya.V. Burgart
Postovsky Institute of Organic Synthesis, Urals Branch of Russian Academy of Sciences, 22/20, S. Kovalevskoy/Akademicheskaya str., Yekaterinburg, 620990 Russia
V.I. Saloutin
Postovsky Institute of Organic Synthesis, Urals Branch of Russian Academy of Sciences, 22/20, S. Kovalevskoy/Akademicheskaya str., Yekaterinburg, 620990 Russia

Abstract

In clinical practice, a large number of prodrugs and active drugs containing an ester, carbamate or amide moiety are used. Carboxylesterase (CaE, EC 3.1.1.1) is the key enzyme of hydrolytic metabolism of such drugs in the body, it largely determines their pharmacokinetics, bioavailability, efficacy and possible toxic effects. Using CaE selective inhibitors as components of combined drug therapy it is possible us to regulate the rate of hydrolytic transformation of ester-containing drugs and opens the possibility of their rational use. The development of effective and selective CaE inhibitors suitable for in vivo application is a new promising approach in medicinal chemistry and pharmacology that allows to improve the efficacy, bioavailability and reduce the side effects of ester-containing drugs.

Article Details

How to Cite
Boltneva, N., Makhaeva, G., Shchegol’kov, E., Burgart, Y., & Saloutin, V. (2018). Selective Carboxylesterase Inhibitors for Improving Efficacy, Safety and Rational use of Ester-Containing Drugs. Biomedical Chemistry: Research and Methods, 1(3), e00026. https://doi.org/10.18097/BMCRM00026
Issue
Vol. 1 No. 3 (2018)
Section
REVIEWS

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