Beta ₂ - Adrenergic Receptor Agonist Studies On Ethanol Amine Compounds Of

In this paper, the pathogenesis of the asthma was described concisely, the structure of β2-adrenoceptor and the reaction mechanism of the 1 -phenyl-2-amino ethanols β2-adrenoceptor agonists were introduced systematically on the molecular level, the development and structure- activity relationship of these β2 -adrenoceptor agonists were reviewed. On the basis of structure-activity relationship of the 1 -phenyl-2-amino ethanols β 2-adrenoceptor agonists , seventeen derivatives of 2-phenyl-2-amino ethanols were designed and synthesized by the principle of isosterism, under considering the high efficiency, high selectivity of the 2-phenyl-2-amino ethanols β2-adrenoceptor agonist SPFF discovered by our group.Other six compounds of JL-018 to JL-023 were 1-phenyl-2-amino ethanols β2-adrenoceptor agonists. Moreover , JL-024 of 4-nitrophenyl ethanolamine was designed and synthesized in order to investigate the reaction mechanism of the epoxyethane. JL-012 to JL-017 were the isomeric compounds of JL-018 to JL-023 respectively. The structures of the compounds were discussed from the reaction mechanism and the differences of spectrum. And all compounds were identified by IR, 1H-NMR and MS. Primary pharmacological tests showed that twenty four target compounds(JL-001 to JL-024) all had moderate relaxing activity on the contracting bronchial smooth muscle of guinea-pigs induced by histamine. Based on the preliminary bioactive data, the QSAR of these compounds were studied by CoMFA for direction of futher modification to the 2-phenyl-2-amino ethanols β2-adrenoceptor agonists.