Synthesis And β Phenylethanolamine Compounds ₂ - Receptor Agonist Activity

In this thesis, the pathogenesis of the asthma, the structrure ofβ₂-adrenoceptor and the action mechanism ofβ₂-adrenoceptor agonists were introduced concisely. At the same time, the development and structure-activity relationship ofβ₂-adrenoceptor agonists are reviewed. According to the structure-activity relationship ofβ₂-adrenoceptor agonists, 21 derivatives of phenylethanolamines, including 7 derivatives （H01-H07） as 1-phenyl-2-amino-ethanols and 14 derivatives （H08-H21） as 2-phenyl-2-amino-ethanols, were designed and synthesized on the principle of isosterism with tranditerol, as a high efficiency, high selectivity and specialty of leading compound. All compounds were characterized by ¹H-NMR and MS, in which H01 and H07 were the isomeric compounds of H14 and H17 respectively. The two types structures were conformed from the differences of their spectra by the two compounds of H07 and H17. Furthermore, the mechanism of the reactions forming the two types of compounds was discussed also.Preliminary pharmacological tests showed that all compounds had relaxing activity on the contracting bronchial smooth muscle of guinea-pigs induced by histamines.Moreover, three dimensional quantitative structure-activity relationship （3D-QSAR） of the synthetic compounds was studied via Comparative Molecular Field Ananlysis （CoMFA）. The result of QSAR can direct further structure modification of 2-phenyl-2-amino ethanols asβ₂-adrenoceptor agonists.