Structure-activity studies on a potent antagonist to organophosphate-induced toxicity
| Autor: | Joseph G. Cannon, Jan R. Flynn, John P. Long, Ranbir K. Bhatnagar, M. Fethi Sahin |
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| Rok vydání: | 1991 |
| Předmět: |
Male
chemistry.chemical_classification Cholinesterase Reactivators Ketone Paraoxon Chemistry Stereochemistry Organophosphate Acetal Antagonist Hemicholinium 3 Lethal Dose 50 Ring size Mice Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Toxicity medicine Animals Molecular Medicine Structure–activity relationship medicine.drug |
| Zdroj: | Journal of Medicinal Chemistry. 34:1582-1584 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00109a009 |
| Popis: | Molecular modifications have been made on a highly potent, active antagonist to organophosphate-induced toxicity, 4,4'-bis[1,3-dioxan-2-ylmethyl)methylamino]acetyl]biphenyl dimethobromide (1). Stepwise removal of the oxygen atoms from the dioxane rings, as well as changing the position of attachment of substituents on the 1,3-dioxane rings and decreasing the ring size from six-membered to five-membered caused drastic or complete loss of pharmacological effect. Partial structures of 1 were all inactive. Thus, the structure of 1 seems to be remarkably specific. Additional pharmacological data are reported for 1. |
| Databáze: | OpenAIRE |
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