Synthesis and evaluation of (piperidinomethylene)bis(phosphonic acid) derivatives as anti-osteoporosis agents.

Abstract:

: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.

authors

Mimura M,Hayashida M,Nomiyama K,Ikegami S,Iida Y,Tamura M,Hiyama Y,Ohishi Y

doi

10.1248/cpb.41.1971

subject

Has Abstract

pub_date

1993-11-01 00:00:00

pages

1971-86

issue

11

eissn

0009-2363

issn

1347-5223

journal_volume

41

pub_type

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