Az eszterhidrolizis kinetikajanak szubmolekularis jellemzese

Translated title of the contribution: Characterization of the kinetics of ester hydrolysis at the submolecular level

Béla Noszál, Márta Kraszni, Dóra Visky

Research output: Contribution to journalArticle

1 Citation (Scopus)

Abstract

Ester-type compounds are important drugs as directly binding active principles, but also, as prodrugs that provide the acting agent after hydrolytic decomposition. The profound characterisation of the kinetics of ester hydrolysis is therefore equally important to interpret and design metabolic processes and prodrug → drug transitions. The extramolecular factors (temperature, ionic strength, solvent etc.) influencing the rate constant values have extensively been studied. Contrary to that, few data can be found on the effect and magnitude of the intramolecular factors (substituent effect, neighbour-group protonation). This paper reports the introduction and determination of microscopic rate constants of ester hydrolysis, a new physicochemical parameter, which is defined in the sense of the protonation state of the basic site(s) adjacent the ester group The microscopic rate constants of phenylalanine-methyl-ester hydrolysis are determined and interpreted. Also, the principles to characterise the rate of monobasic double esters at the submolecular level, exemplified by cocaine, are established.

Translated title of the contributionCharacterization of the kinetics of ester hydrolysis at the submolecular level
Original languageHungarian
Pages (from-to)147-154
Number of pages8
JournalActa pharmaceutica Hungarica
Volume69
Issue number3
Publication statusPublished - Jun 1 1999

ASJC Scopus subject areas

  • Pharmaceutical Science

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