| Summary: | 碩士 === 中國醫藥大學 === 藥物化學研究所碩士班 === 94 === A series of ethyl 2-[N-substituted benzyl- 4´(or 3´)-bromo]anilino-
4-oxo-4,5-dihydrofuran-3-carboxylate and related compounds has been synthesized and assigned by their spectra data. All of these synthetic compounds were evaluated for anti-arrhythmics activity and cardiovascular effect.
Among the investigations of the inhibitory effect on the heart rate , Ethyl 2-[N-m-fluorobenzyl-(3´-bromo)]anilino-4-oxo-4,5-dihydrofuran-3-carboxylate
（27）、Ethyl 2-[N-m-chlorobenzyl-(3´-bromo)]anilino-4-oxo-4,5-dihydro-
furan-3-carboxylate（30）、Ethyl 2-[N- benzyl-(3´-bromo)]anilino-4-oxo-
4,5-dihydrofuran-3-carboxylate（19）were found to exhibit the most significant activities at 30 μM while pacermaker S.A. node. Ethyl 2-[N-
benzyl-(4´-bromo)] anilino-4-oxo-4,5-dihydrofuran-3-carboxylate（2），Ethyl 2-[N-m-methylbenzyl-(4´-bromo)]anilino-4-oxo-4,5-dihydrofuran-
3-carboxylate（4），Ethyl 2-[N-m-fluorobenzyl-(4´-bromo)]anilino-4-oxo-
4,5-dihydrofuran-3-carboxylate（10），Ethyl 2-[N-m-chlorobenzyl-(4´-
bromo)]anilino-4-oxo-4,5-dihydrofuran-3-carboxylate（13），Ethyl 2-[N-o-nitrobenzyl-(4´-bromo)]anilino-4-oxo-4,5-dihydrofuran-3-
carboxylate（15），Ethyl 2-[N-p-nitrobenzyl-(4´-bromo)]anilino-4-oxo-
4,5-dihydrofuran-3-carboxylate（17），Ethyl 2-[N-o-methylbenzyl-
(3´-bromo)]anilino-4-oxo-4,5-dihydrofuran-3-carboxylate（20），Ethyl
2-[N-p-chlorobenzyl-(3´-bromo)]anilino-4-oxo-4,5-dihydrofuran-3-
carboxylate（31），Ethyl 2-[N-o-nitrobenzyl-(3´-bromo)]anilino-4-oxo-4,5-
dihydrofuran-3-carboxylate（32）exhibited better activities and no inhibitory effect on the pacemaker S.A. node. Ethyl 2-[N-m-methyl benzyl-(3´-bromo)]anilino-4-oxo-4,5-dihydrofuran-3-carboxylate（21）
and Ethyl 2-[N-p-methoxybenzyl-(3´-bromo)]anilino-4-oxo-4,5-dihydro-
furan-3-carboxylate（24）also exhibited a better inhibitory effect at
10μM，but inhibition to pacemaker S.A. node. occurred at concentrations up to 30 μM.
Among the results of the contractivity , ethyl 2-[N-m-methylbenzyl-
(4´-bromo)]anilino-4-oxo-4,5-dihydrofuran-3-carboxylate（4），Ethyl 2-[N-
m-methoxybenzyl-(4´-bromo)]anilino-4-oxo-4,5-dihydrofuran-3-carboxylate
（7），Ethyl 2-[N-p-methoxybenzyl-(4´-bromo)]anilino-4-oxo-4,5-dihydro-
furan-3-carboxylate（8），Ethyl 2-[N-m- fluorobenzyl-(4´-bromo)]anilino-
4-oxo-4,5-dihydrofuran-3-carboxylate（10）and Ethyl 2-[N-p- methoxyl benzyl-(3´-bromo)]anilino-4-oxo-4,5-dihydrofuran-3-carboxylate（25）
exhibited better activities.
In conclusion, most of this series of compounds basically exhibited activities of increasing contractility and lowering heart rate.
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