Novel Basic Isoflavones as Inhibitors of Bone Resorption
摘要:
A number of aminoalkoxy analogues of ipriflavone (=7-(1-methylethoxy)isoflavone) were prepared and examined for their capacity to inhibit bone resorption induced by bovine parathyroid hormone fragment 1 - 34. Good-to-high activities were found for 7-(aminoalkoxy)isoflavone. analogues. Their activity was influenced by a number of structural features, among which the length of the basic side chain, the basicity of the amino group, and the nature and position of substituents on the 3-phenyl ring. 4'-(Aminoalkoxy)ipriflavone derivatives were less active.
A FACILE SYNTHESIS OF ANGULAR AND LINEAR 8/2-METHYL-FURO[2,3-h]/[3,2-g] CHROMONES AND ANGULAR PYRANO[2,3-f] ISOFLAVONES FROM 7-PROPARGYLOXY CHROMONES AND ISOFLAVONES
(2). 2a under the thermal conditions of the reaction, undergoes [3,3] sigmatropicshift to give 7-hydroxy-8allenyl chromone (5a). The chromone carbonyl which is para to the hydroxyl ionizes the hydroxyl group, thereby generating a stable polar intermediate (6a). Kinetically controlled nucleophilic attack by the hydroxyl at the allene C-2 give rise to five membered methyl furan ring (3a). Scheme-l