Structural requirements for the sequestration of metabolically generated acetaldehyde
- 1 February 1980
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 23 (2), 140-143
- https://doi.org/10.1021/jm00176a007
Abstract
Of a series of polyfunctional compounds containing amino, hydroxyl, or mercapto groups in conjunction with the carboxyl group, only the 1,2- or 1,3-disubstituted aminothiols, i.e., D-(-)-penicillamine (1), L-cysteine, L-cysteinyl-L-valine, mercaptoethylglycine, and DL-homocysteine, showed any propensity to sequester acetaldehyde (AcH) when tested in vitro in a buffered system at pH 7.5. In vivo only 1 was effective in lowering ethanol-derived blood AcH in rats that had been treated with disulfiram and ethanol. In addition to the functionality in the molecule, pharmacokinetic and metabolic factors must also be considered when designing AcH-sequestering agents for use in vivo.This publication has 6 references indexed in Scilit:
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