Comparative QSAR and radical toxicology: the aromatic CH2OH moiety

Autor:	Rajni Garg, Corwin Hansch
Rok vydání:	2001
Předmět:	Quantitative structure–activity relationship Lucanthone Stereochemistry Metabolite Chloramphenicol Radical Conjugated system Toxicology chemistry.chemical_compound chemistry medicine Moiety medicine.drug Methyl group
Zdroj:	Journal of the Chemical Society, Perkin Transactions 2. :476-479
ISSN:	1364-5471 1472-779X
Popis:	Evidence is summarized to show via quantitative structure–activity relationships (QSAR) that the aromatic CH2OH group when conjugated with electron-releasing substituents displays toxic effects that suggest a radical reaction mechanism. The evidence can be used to explain the inhibitory action of lucanthone toward schistosomiasis. That is, lucanthone per se is not active, but its metabolite in which a methyl group has been converted to CH2OH is. This calls to mind the activity of chloramphenicol, which was a very effective anti-bacterial agent, but also caused serious blood dyscrasias in some patients. Presumably this could have been due to the toxic action of radicals.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::1a2d737cf0f0fa82b3e974af7b09e9de https://doi.org/10.1039/b010085o Zobrazit plný text záznamu