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[Studies on the synthesis and bioactivity of alpha-alkylaminobenzyl-phosphonic acids]
1Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, China. wangdx@imm.ac.cn
Aim:
To search for some substituted benzyl phosphonic acids as leading compounds with inhibiting effect on osteoclast formation.
Methods:
Target compounds were prepared from aromatic aldehydes, primary amine and phosphorous acid using tetramethylenesulfone as solvent via Arbuzov type reaction. The effect on inhibiting the formation of osteoclast-like cells (OLC) of related compounds was studied by incubating the extract of rat femur marrow.
Results:
Ten compounds of alpha-alkylaminobenzyl phosphonic acids have been synthesized and identified by MS or 1HNMR analysis. Three (2, 8 and 9) of them were found to have notable effect on the inhibition of OLC formation (P < 0.01).
Conclusion:
Among the present substituted benzyl phosphonic acids, the increased aromaticity and hydrophobicity (such as compound 9) can remarkably enhance the ability to inhibit OLC formation.