Nine sulphur and selenium heterosubstituted isomers of N,N-diethylcarbamylcholine and carbaryl have been prepared and their inhibiting activity towards electric eel acetylcholinesterase (E.C. 3.1.1.7) have been measured. The N,N-diethylcarbamylcholines acted only as reversible inhibitors, i.e. they could not carbamylate the enzyme. The reversible inhibition was of mixed type. Sulphur and selenium substitution had only marginal effects on Ki(0.2-0.3 mM) but reduced the value of K'i. The heterosubstituted carbaryl analogues were, with one exception, found to be irreversible inhibitors, about 100 times less potent than carbaryl.
The synthesis of eleven 4‐(5)arylethenylimidazoles and their separation into cis and trans isomers is described. Ir, uv, nmr, and mass spectrometric data of the compounds are given. The photocyclization of the unsubstituted and p‐substituted compounds is reported.
Bei der Kondensation des Phosphoniumsalzes (I) mit Imidazol‐2‐aldehyd (II) entstehen die Olefine (III), die photochemisch zu den Tricyclen (IV) kondensiert werden.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.