Study On The Design, Synthesis And Activity Of Novel Phenylethanolamine Compounds

In this thesis, the pathogenesis, the curatives of the asthma and the action mechanism ofβ2-adrenoceptor agonists were described concisely, and the develop-ment ofβ2-adrenoceptor agonists were introduced detailedly.Based on the structure-activity relationship of our group’s former studies on phenylethanolamine compounds, eighteen derivatives of 2-amine-2-phenylethanol were designed and synthesized on Molecular Field Similarity Analysis Method, with considering the efficiency, selectivity of tranditerol. The final compounds include five series:4-amino-3-phenylsulfonylphenylethanolamine; 4-amino-3-bromo-5-phenylsul-fonylphenylethanolamine; 4-amino-3-chloro-5-phenylsulfonylphenylethanolamine,4-amino-3-bromo-5-methyllsulfonylphenylethanolamine and 4-amino-3-chloro-5-met-hylsulfonylphenylethanolamine. All the novel compounds were identified by 1H-NMR and MS.Priliminary pharmacological tests showed that eighteen compounds (GDD-01-GDD-18) had different relaxing activities on the contracting bronchial smooth muscle of guinea-pigs induced by histamine. Among these compounds, GDD-15 and GDD-17 displayed high activities.