SYNTHESIS AND ANTIOSTEOPOROSIS ACTIVITY OF 3-PHENYL-4(1H) QUINOLINONE DERIVATIVES

AIMTo design and synthesize 7-hydroxy-3-(substituted) phenyl-4(1H) quinolinone and 5-hydroxy-3-(substituted) phenyl-4(1H) quinolinone and to study the antiosteoporosis activity of these compounds. METHODSThe compounds of 7-hydroxy and 5-hydroxy were prepared simultaneously by improved Gould-Jacobs reaction and resorcin was used as starting material. Eight compounds (A_1～4, B_1～4) were synthesized and their chemical structures were determined by IR, MS, ¹HNMR and elemental analysis. Their osteoplastic activity was evaluated by the absorptive test to Ca²⁺ of hydroxyapatite crystal. RESULTSCompounds (A_1～4,B_1～4) are new compounds. Compounds B₁ and B₂ showed antiosteoporosis activities and was stronger than the control drug of tetracycline. CONCLUSIONCompounds B₁ and B₂ are worthy to be intensively studied.