药物化学综实验论文 - 沈阳药科大学精品课程建设.pptVIP

Paper for the Opened-Experiment of Medicinal Chemistry ——Structure-Activity Study of β-Adrenergic Blockers and Laboratory Synthesis of Practolol Compounds that act as blockers of a receptor should possess the structural features of an agonist that contribute to affinity an not those that contribute to intrinsic activity. It is therefore not surprising that a structural prerequisite for beta antagonism is the phenethanol-amino structure and a hydrophobic group (isopropyl or larger) on the nitrogen. To eliminate intrinsic activity in a direct agonist, the phenolic hydroxyl groups of norepineph