SYNTHESIS AND EVALUATION OF (PIPERIDINOMETHYLENE)BIS(PHOSPHONIC ACID) DERIVATIVES AS ANTI-OSTEOPOROSIS AGENTS

被引：0

作者：

MIMURA, M ^{[1
]}

HAYASHIDA, M ^{[1
]}

NOMIYAMA, K ^{[1
]}

IKEGAMI, S ^{[1
]}

IIDA, Y ^{[1
]}

TAMURA, M ^{[1
]}

HIYAMA, Y ^{[1
]}

OHISHI, Y ^{[1
]}

机构：

[1] KAKEN PHARMACEUT CO LTD, CENT RES INST, 14 MINAMIKAWARA MACHI SHINOMIYA, YAMASHINA KU, KYOTO 607, JAPAN

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 1993年 / 41卷 / 11期

关键词：

BONE RESORPTION; OSTEOPOROSIS; HYPERCALCEMIA; SERUM CALCIUM; BISPHOSPHONATE; (4-SUBSTITUTED PIPERIDINOMETHYL-ENE)BIS(PHOSPHONIC ACID);

D O I：

暂无

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Some (piperidinomethylene)bis(phosphonic acid) derivatives were prepared and their activity to inhibit a rise in serum calcium induced by parathyroid hormone in thyroparathyroidectomised rats was evaluated. Several (4-alkylidene-, 4,4-dialkyl-, or 4-alkyl-4-halopiperidinomethylene)bis(phosphonic acid) derivatives showed considerable inhibitory activity. But compounds having aromatic and polar substituents such as azido, hydroxy, amino and amido on the piperidine ring were generally inactive. In this study, two 4-alkylidene compounds (8a and 8b) and a 4,4-cyclic dialkyl compound (61) showed potent activity when administered either intravenously or perorally.

引用

页码：1971 / 1986

页数：16

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