| 摘要: | 著者合成了一系列 2-(氮-取代?基)?啶胺基-4-酮基-4,5-二氫?喃-3-羧酸乙酯化合物，且經各種圖譜資料予以確認之後，將所有合成經結構判定正確之化合物分別測試其抗心律不整與抗癌活性。 在心律測試方面，化合物Ethyl 2-[N-o-methoxybenzyl-(5￠- methylpyridyl)]amino-4-oxo-4,5-dihydrofuran-3-carboxylate（22）在30μM活性最強，但在100μM會抑制右心房自發性節律；化合物Ethyl 2-(N-m-chlorobenzyl)pyridylamino-4-oxo-4,5-dihydrofuran-3- carboxylate（4），Ethyl 2-(N-p-chlorobenzyl)pyridylamino-4-oxo-4,5- dihydrofuran-3-carboxylate（5），Ethyl 2-(N-o-methoxybenzyl)pyridyl amino-4-oxo-4,5-dihydrofuran-3-carboxylate（9），Ethyl 2-(N-p-methyl benzyl)pyridylamino-4-oxo-4,5-dihydrofuran-3-carboxylate（13）呈現較佳之抑制活性，且不會抑制右心房自發性節律。 而在強心測試方面，其中化合物Ethyl 2-(N-p-chlorobenzyl) pyridylamino-4-oxo-4,5-dihydrofuran-3-carboxylate（5），Ethyl 2-(N-o-methoxybenzyl)pyridylamino-4-oxo-4,5-dihydrofuran-3- carboxylate（9），Ethyl 2-(N-m-methoxybenzyl)pyridylamino-4-oxo-4,5- dihydrofuran-3-carboxylate（10），Ethyl 2-(N-p-methoxybenzyl) pyridylamino-4-oxo-4,5-dihydrofuran-3-carboxylate（11），Ethyl 2-[N-benzyl-N-(5’-methylpyridyl)]amino-4-oxo-4,5-dihydrofuran-3- carboxylate（15），Ethyl 2-[N-o-chlorobenzyl-(5￠-methylpyridyl)]amino- 4-oxo-4,5-dihydrofuran-3-carboxylate（16），Ethyl 2-[N-m-chlorobenzyl-(5￠-methylpyridyl)]amino-4-oxo-4,5-dihydrofuran- 3-carboxylate（17），Ethyl 2-[N-p-chlorobenzyl-(5￠-methylpyridyl)] amino-4-oxo-4,5-dihydrofuran-3-carboxylate（18），Ethyl 2-[N-o- fluorobenzyl-(5￠-methylpyridyl)]amino-4-oxo-4,5-dihydrofuran-3- carboxylate（19），Ethyl 2-[N-m-fluorobenzyl-(5￠-methylpyridyl)] amino-4-oxo-4,5-dihydrofuran-3-carboxylate（20），Ethyl 2-[N-m-methoxybenzyl-(5￠-methylpyridyl)]amino-4-oxo-4,5-dihydro- furan-3-carboxylate（23），Ethyl 2-[N-p-methoxybenzyl-(5￠- methylpyridyl)]amino-4-oxo-4,5-dihydrofuran-3-carboxylate（24），Ethyl 2-[N-m-methylbenzyl-(5￠-methylpyridyl)]amino-4-oxo-4,5-dihydrofuran-3-carboxylate（26）在強心方面有較好之藥理活性。 對乳癌細胞（MCF 7）、肺癌細胞（NCI-H460）、星細胞瘤（SF-268）與子宮頸細胞株( HeLa )的生長抑制活性： 實驗後發現Ethyl 2-(N-p-methoxybenzyl)pyridylamino-4-oxo-4,5- dihydrofuran-3-carboxylate（11）對乳癌細胞（MCF 7）、肺癌細胞（NCI-H460）有較好抑制活性。 Ethyl 2-[N-o-chlorobenzyl-(5￠- methypyridyl)]amino-4-oxo-4,5-dihydrofuran-3-carboxylate（16）對子宮頸細胞株( HeLa )有較好抑制活性。Ethyl 2-[N-o-methoxybenzyl-(5￠- methylpyridyl)]amino-4-oxo-4,5-dihydro furan-3-carboxylate（22）對乳癌細胞（MCF 7）、肺癌細胞（NCI-H460）、星細胞瘤（SF-268）與子宮頸細胞株( HeLa )均有較好抑制活性，而其他化合物並無明顯抑制活性。 總結，本系列化合物(5)和(9)皆具有增加心收縮力與減慢心跳頻律作用；而化合物(4)和(13)具有減慢心跳頻律作用；化合物(10)、(11)、(15)、(16)、(17)、(18)、(19)、(20)、(23)、(24)和(26)具有增加心收縮力作用；而化合物（11）、（16）和（22）具有細胞毒性作用。; A series of Ethyl 2-(N-substituted benzyl)pyridylamino-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-arrhythmias activity and anticancer effect. Among the investigations of the inhibitory effect on the heart rate , Ethyl 2-[N-o-methoxybenzyl-(5￠-methylpyridyl)]amino-4-oxo-4,5- dihydrofuran-3-carboxylate（22）was found to exhibit the most significant activities at 30μM while pacermaker S.A. node was inhibited at concentrations up to 100 μM. Ethyl 2-(N-m-chlorobenzyl)- pyridylamino-4-oxo-4,5-dihydrofuran-3-carboxylate（4），Ethyl 2-(N-p- chlorobenzyl)pyridylamino-4-oxo-4,5-dihydrofuran-3-carboxylate（5），Ethyl 2-(N-o-methoxybenzyl)pyridylamino-4-oxo-4,5-dihydrofuran-3- carboxylate（9），Ethyl 2-(N-p-methylbenzyl)pyridylamino-4-oxo-4,5- dihydrofuran-3-carboxylate（13）exhibited better activities and no inhibitory effect on the pacemaker S.A. node. Among the results of the contractivity , Ethyl 2-(N-p-chlorobenzyl)- pyridylamino-4-oxo-4,5-dihydrofuran-3-carboxylate（5），Ethyl 2-(N-o- methoxybenzyl)pyridylamino-4-oxo-4,5-dihydrofuran-3-carboxylate（9），Ethyl 2-(N-m-methoxybenzyl)pyridylamino-4-oxo-4,5-dihydrofuran- 3-carboxylate（10），Ethyl 2-(N-p-methoxybenzyl)pyridylamino- 4-oxo-4,5-dihydrofuran-3-carboxylate（11），Ethyl 2-[N-benzyl-N-(5’- methylpyridyl)]amino-4-oxo-4,5-dihydrofuran-3-carboxylate（15），Ethyl 2-[N-o-chlorobenzyl-(5￠-methylpyridyl)]amino-4-oxo-4,5-dihydrofuran-3- carboxylate（16），Ethyl 2-[N-m-chlorobenzyl-(5￠-methylpyridyl)]amino- 4-oxo-4,5-dihydrofuran-3-carboxyla |
