1690-75-1Relevant articles and documents
Approaches to Protection against Nerve Agent Poisoning. (Naphthylvinyl)pyridine Derivatives as Potential Antidotes
Gray, Allan P.,Platz, Robert D.,Henderson, Theresa R.,Chang, Timothy C. P.,Takahashi, Kazuyuki,Dretchen, Kenneth L.
, p. 807 - 814 (1988)
Analogues of the potent inhibitor of choline acetyltransferase (CAT) (E)-4-(1-naphthylvinyl)pyridine methiodide were synthesized and evaluated for their ability to inhibit CAT and protect against nerve agent intoxication.Several compounds, notably (E)-1-(2-hydroxyethyl)-(1-naphthylvinyl)pyridinium bromide (3), (E)-1-methyl-4-(1-naphthylvinyl)-1,2,3,6-tetrahydropyridine hydrochloride (22), and (E)-1-methyl-4-(1-naphthylvinyl)piperidine hydrochloride (23), were found to afford significant protection against sarin in the mouse and against soman in the giunea pig.However, protection was apparently not related to CAT inhibition.Compound 23, our most effective compound in protecting against nerve agent, was without CAT inhibitory activity.Compound 22, which proved to be a potent CAT inhibitor, most likely owed this activity to being dehydrogenated back to the pyridinium quaternary salt by oxidative enzymes.Several of the (naphthylvinyl)pyridine quaternary salts, but not their tertiary amine analogues, were found to be effective in slowing the rate of aging of soman-inhibited acetylcholinesterase.Ability to slow the rate of aging was enhanced by introduction of methoxy substituents on the aryl moiety whereas the aging rate was actually accelerated by chloro substituents.To date, our most effective compound in slowing the rate of aging, (E)-4-pyridine methochloride (6), did not provide significant protection against soman in the mouse.
COMPOUND LIBRARIES OF N-(AMINOCARBONYL)-PIPERIDINE-4-CARBOXAMIDE DERIVATIVES CAPABLE OF BINDING TO G-PROTEIN COUPLED RECEPTORS
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Page/Page column 26-27, (2008/06/13)
The present invention provides a compound library targeted to receptors with a requirement for a positively charged amine in their structure activity relationships. It is designed to produce both agonists and antagonists and so is expected to be especially useful in producing ligands for orphan receptors. The library is designed around an acylurea coupled to a piperidine moiety. A combination of specific motifs R2 and R1 are appended from the central scaffold and are designed to pick up different interactions at a receptor site. The library comprises or consists of a set of structurally related compounds of general formula (I).
Anti-hypertensive piperidine compounds
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, (2008/06/13)
Novel compounds of the formula: STR1 are described wherein Z is a bicyclic aryl group containing between 9 and 10 ring atoms, up to two of which may be nitrogen and up to one of which may be oxygen or sulfur; A is an ethenyl group which may be lower-alkyl-substituted; and R and R' each represent H or an aliphatic group of 1-4 carbon atoms; or a pharmaceutically acceptable acid addition salt thereof.