著者

森田 岩男 国本 克俊 津田 正己 但田 信一 黄瀬 正博 木村 喜代史

出版者

公益社団法人日本薬学会

雑誌

Chemical & pharmaceutical bulletin (ISSN:00092363)

巻号頁・発行日

vol.35, no.10, pp.4144-4154, 1987-10-25

---

A series of 1,4-dihydropyridine-5-cyclic phosphonate derivatives, designed as analogues of 1,4-dihydropyridine-3,5-dicarboxylate calcium antagonists, was synthesized and examined for antihypertensive activity. Several compounds were proved to have activities superior or comparable to that of nifedipine in lowering blood pressure in normotensive and spontaneously hypertensive rats (SHR). Among these compounds, methyl 2,6-dimethyl-5-(2-oxo-1,3,2-dioxaphosphorinan-2-yl)-4(2-nitrophenyl)-1,4-dihydropyridine-3-carboxylate (31, DHP-218) was approximately 7 times more active than nifedipine in SHR and was selected for further development and clinical evaluation. The structure-activity relationships are discussed.

著者

倉 紘平 福井 久司 福井 孝子 岡本 美由紀 田島 小雪 黒坂 智恵美 林 誠治 藤沢 広 井上 吉郎 鵜飼 洋司郎 上田 房雄 吉國 義明 木村 喜代史

雑誌

日本化学療法学会雜誌 = Japanese journal of chemotherapy (ISSN:13407007)

巻号頁・発行日

vol.44, pp.113-128, 1996-03-01

参考文献数

15

被引用文献数

1