苏州大学医学部药学院 教 案 课程名称： Medicinal Chemistry 授课对象： 药学（全英文方向）3年级 授课学时： 90学时 Foye's Principles of 教材版本： Medicinal Chemistry, 7th edition 主讲教师： 乔春华，仇晓琰，叶娜 苏州大学医学部药学院制 2020年9月12日
苏州大学医学部药学院 教 案 课程名称： Medicinal Chemistry 授课对象： 药学（全英文方向）3 年级 授课学时： 90 学时 教材版本： Foye’s Principles of Medicinal Chemistry, 7th edition 主讲教师： 乔春华，仇晓琰，叶娜 苏州大学医学部药学院制 2020 年 9 月 12 日
苏州大学医学部药学院授课教案 授课教师：叶娜 授课日期：2020.9.18,9.22 课程名称 Medicinal Chemistry 所属学科 药学 医18药学3 教材名称 Foye's Principles of Medicinal Chemistry, 7th edition 授课年级 (全英文方 向) Chapter 3.Physicochemical and 授课章节 Biopharmaceutical Properties of Drug 授课时间 4课时 Substances 、 教学目标：含知识目标、技能（能力）目标 1.知识目标： (1) Get a general idea about Physiochemical and Biopharmaceutical Properties of Drug Substances; (2) Understand the relationship of physiochemical and biopharmaceutical factors of drugs and ADME (3) Get a general idea about Pharmacokinetics; (4) To master how to be druglike 2.技能（能力）目标：结合实验课程目标
苏州大学医学部药学院授课教案 授课教师： 叶娜 授课日期：2020.9.18，9.22 课程名称 Medicinal Chemistry 所属学科 药学 教材名称 Foye’s Principles of Medicinal Chemistry, 7th edition 授课年级 医 18 药学 3 （全英文方 向） 授课章节 Chapter 3. Physicochemical and Biopharmaceutical Properties of Drug Substances 授课时间 4 课时 一、 教学目标：含知识目标、技能（能力）目标 1. 知识目标： （1） Get a general idea about Physiochemical and Biopharmaceutical Properties of Drug Substances; （2） Understand the relationship of physiochemical and biopharmaceutical factors of drugs and ADME （3） Get a general idea about Pharmacokinetics; （4） To master how to be druglike 2. 技能（能力）目标：结合实验课程目标
二 授课内容（依据教学大纲）及时间分配 Get a general idea about Fate of Drugs in Body 8min Get a general idea about Pharmacokinetics and Pharmacodynamics 7min Get a general idea about trends of attrition rates in drug development, and purposes of PK study 10 min To master the relationship of physiochemical and biopharmaceutical factors of drugs and ADME(75 min) Drug Absorption 40 min Drug Distribution 20 min Drug Metabolism 10 min Drug Excretion 5min Pharmacokinetics(60 min) Plasma drug concentration-time curves 15 min Basic PK parameters(V,Cl,T1/2,F,AUC) 45 min How to be druglike(40 min) Optimization of physiochemical and biopharmaceutical properties 10 min Optimization of Pharmacokinetic Profiles 20 min How to Mitigate the Risk of Drug Toxicity 10 min 三、 教学重点与难点 1. 教学重点 (1)Understand the relationship of physiochemical and biopharmaceutical factors
二、 授课内容（依据教学大纲）及时间分配 Get a general idea about Fate of Drugs in Body 8 min Get a general idea about Pharmacokinetics and Pharmacodynamics 7 min Get a general idea about trends of attrition rates in drug development, and purposes of PK study 10 min To master the relationship of physiochemical and biopharmaceutical factors of drugs and ADME (75 min) Drug Absorption 40 min Drug Distribution 20 min Drug Metabolism 10 min Drug Excretion 5 min Pharmacokinetics (60 min) Plasma drug concentration‐time curves 15 min Basic PK parameters (V, Cl, T1/2, F, AUC) 45 min How to be druglike (40 min) Optimization of physiochemical and biopharmaceutical properties 10 min Optimization of Pharmacokinetic Profiles 20 min How to Mitigate the Risk of Drug Toxicity 10 min 三、 教学重点与难点 1. 教学重点 （1）Understand the relationship of physiochemical and biopharmaceutical factors
of drugs and ADME (2)To master how to be druglike 2.教学难点 (1)Understand the relationship of physiochemical and biopharmaceutical factors of drugs and ADME (2)To master how to be druglike 四、 教学方法选择 1.理论课堂教学 A.多媒体教学： (简要列出本章节多媒体教学设计特点及优势) B.互动教学：（根据实际情况列出案例/实例讨论、分析讨论、分组讨论、翻转课堂 等互动教学内容标题) 2.实验教学： (简要列出实验内容标题)
of drugs and ADME （2）To master how to be druglike 2. 教学难点 （1）Understand the relationship of physiochemical and biopharmaceutical factors of drugs and ADME （2）To master how to be druglike 四、 教学方法选择 1. 理论课堂教学 A. 多媒体教学：（简要列出本章节多媒体教学设计特点及优势） B. 互动教学：（根据实际情况列出案例/实例讨论、分析讨论、分组讨论、翻转课堂 等互动教学内容标题） 2. 实验教学：（简要列出实验内容标题）
五、 更新或补充内容提要 六、 复习思考题 1.How do pKa and lipid solubility affect drug absorption? 2.What is the predominant transport mode for absorption of most commercial drugs? 3.Which of the following structural modifications likely will improve permeability? (a)change an amine to a methyl;(b)add a methoxy groups;(c)remove a propyl group;(d)change a carboxylic acid to en ethyl ester;(e)change a carboxylic acid to a terazole. 4.Which parameters are used to describe PK? 5.Descibe the type of prodrug,the purpose of prodrug design,and provide examples to explain how to design prodrug? 七、 学习资源、课外自主学习参考 (可以列出供学生进一步学习、拓展本章节内容的网站、著作、期肝刊的名称及内容等 《药物化学》尤启冬主编，化学工业出版社，第三版
五、 更新或补充内容提要 六、 复习思考题 1. How do pKa and lipid solubility affect drug absorption? 2. What is the predominant transport mode for absorption of most commercial drugs? 3. Which of the following structural modifications likely will improve permeability? (a) change an amine to a methyl; (b) add a methoxy groups; (c) remove a propyl group; (d) change a carboxylic acid to en ethyl ester; (e) change a carboxylic acid to a terazole. 4. Which parameters are used to describe PK? 5. Descibe the type of prodrug, the purpose of prodrug design, and provide examples to explain how to design prodrug? 七、 学习资源、课外自主学习参考 (可以列出供学生进一步学习、拓展本章节内容的网站、著作、期刊的名称及内容等 《药物化学》尤启冬主编，化学工业出版社，第三版
苏州大学医学部药学院授课教案 授课教师：叶娜 授课日期：2020.9.24 课程名称 Medicinal Chemistry 所属学科 药学 医18药学3 教材名称 Foye's Principles of Medicinal Chemistry, 7th edition 授课年级 (全英文方 向) 授课章节 Chapter 9.Drugs Affecting Cholinergic Neurotransmission 授课时间 2课时 一、 教学目标：含知识目标、技能（能力）目标 1.知识目标： (1)Get a general idea about acetylcholine and cholinergic receptors; Understand the development history of drugs affecting cholinergic neurotransmission; (2)To master the chemical structures,drug design,structure-activity relationships,and mechanism of actions of major drugs affecting cholinergic neurotransmission; (3) Understand the synthesis and metabolism of major drugs affecting cholinergic neurotransmission 2.技能（能力）目标：结合实验课程目标
苏州大学医学部药学院授课教案 授课教师： 叶娜 授课日期：2020.9.24 课程名称 Medicinal Chemistry 所属学科 药学 教材名称 Foye’s Principles of Medicinal Chemistry, 7th edition 授课年级 医 18 药学 3 （全英文方 向） 授课章节 Chapter 9. Drugs Affecting Cholinergic Neurotransmission 授课时间 2 课时 一、 教学目标：含知识目标、技能（能力）目标 1. 知识目标： （1） Get a general idea about acetylcholine and cholinergic receptors; Understand the development history of drugs affecting cholinergic neurotransmission; （2） To master the chemical structures, drug design, structure-activity relationships, and mechanism of actions of major drugs affecting cholinergic neurotransmission; （3） Understand the synthesis and metabolism of major drugs affecting cholinergic neurotransmission 2. 技能（能力）目标：结合实验课程目标
二 授课内容（依据教学大纲）及时间分配 Get a general idea about neurotransmitters and associated neuropsychiatric disease 7min Get a general idea about acetylcholine and its functions and neurochemistry 8min Get a general idea about the distribution,structures and functions of cholinergic receptors 8min Get a general idea about Alzheimer disease 7min To master the chemical structures,drug design,structure-activity relationships,and mechanism of actions of major cholinergic drugs; Understand the synthesis and metabolism of major cholinergic drugs Including the following specific drugs(70 min): Muscarinic Agonists:Methacholine Chloride;Carbachol;Bethanechol Chloride;Pilocarpine;Cevimeline 20 min Acetylcholinesterase Inhibitors:Neostigmine;Rivastigmine;Tacrine; Galantamine;Donepezil; 25 min Muscarinic Antagonists:Atropine and its Analogues;Tiotropium bromide;Artane;Benztropine. 25min 三、 教学重点与难点 1.教学重点 Drug discovery and design,chemical structures,structure-activity relationships,and mechanism of actions of major cholinergic drugs
二、 授课内容（依据教学大纲）及时间分配 Get a general idea about neurotransmitters and associated neuropsychiatric disease 7 min Get a general idea about acetylcholine and its functions and neurochemistry 8 min Get a general idea about the distribution, structures and functions of cholinergic receptors 8 min Get a general idea about Alzheimer disease 7 min To master the chemical structures, drug design, structure-activity relationships, and mechanism of actions of major cholinergic drugs; Understand the synthesis and metabolism of major cholinergic drugs Including the following specific drugs (70 min): Muscarinic Agonists: Methacholine Chloride; Carbachol; Bethanechol Chloride; Pilocarpine; Cevimeline 20 min Acetylcholinesterase Inhibitors: Neostigmine; Rivastigmine; Tacrine; Galantamine; Donepezil; 25 min Muscarinic Antagonists: Atropine and its Analogues; Tiotropium bromide; Artane; Benztropine. 25 min 三、 教学重点与难点 1. 教学重点 Drug discovery and design, chemical structures, structure-activity relationships, and mechanism of actions of major cholinergic drugs
2.教学难点 Drug discovery and design,chemical structures,structure-activity relationships,and mechanism of actions of major cholinergic drugs 四、 教学方法选择 3.理论课堂教学 A.多媒体教学： (简要列出本章节多媒体教学设计特点及优势) B.互动教学：（根据实际情况列出案例/实例讨论、分析讨论、分组讨论、翻转课堂 等互动教学内容标题) 4.实验教学： (简要列出实验内容标题) 五、 更新或补充内容提要
2. 教学难点 Drug discovery and design, chemical structures, structure-activity relationships, and mechanism of actions of major cholinergic drugs 四、 教学方法选择 3. 理论课堂教学 A. 多媒体教学：（简要列出本章节多媒体教学设计特点及优势） B. 互动教学：（根据实际情况列出案例/实例讨论、分析讨论、分组讨论、翻转课堂 等互动教学内容标题） 4. 实验教学：（简要列出实验内容标题） 五、 更新或补充内容提要
六 复习思考题 Write down the chemical structual of acetylcholine.Can patients with deficiencies in acetylcholine could be treated by administering acetylcholine itself?Why? 七、 学习资源、课外自主学习参考 (可以列出供学生进一步学习、拓展本章节内容的网站、著作、期肝刊的名称及内容等) 《药物化学》尤启冬主编，化学工业出版社，第三版
六、 复习思考题 Write down the chemical structual of acetylcholine. Can patients with deficiencies in acetylcholine could be treated by administering acetylcholine itself? Why? 七、 学习资源、课外自主学习参考 (可以列出供学生进一步学习、拓展本章节内容的网站、著作、期刊的名称及内容等) 《药物化学》尤启冬主编，化学工业出版社，第三版
苏州大学医学部药学院授课教案 授课教师：叶娜 授课日期：2020.9.25 课程名称 Medicinal Chemistry 所属学科 药学 医18药学3 教材名称 Foye's Principles of Medicinal Chemistry, 7th edition 授课年级 (全英文方 向) Chapter 10.Adrenergic Receptors and 授课章节 Drugs Affecting Adrenergic 授课时间 2课时 Neurotransmission 一、 教学目标：含知识目标、技能（能力）目标 3.知识目标： (1) Get a general idea about adrenaline and adrenergic receptors;Understand the development history of drugs affecting adrenergic neurotransmission; (2) To master the chemical structures,drug design,structure-activity relationships,and mechanism of actions of major drugs affecting adrenergic neurotransmission; (3)Understand the synthesis and metabolism of major drugs affecting adrenergic neurotransmission 4.技能（能力）目标：结合实验课程目标
苏州大学医学部药学院授课教案 授课教师： 叶娜 授课日期：2020.9.25 课程名称 Medicinal Chemistry 所属学科 药学 教材名称 Foye’s Principles of Medicinal Chemistry, 7th edition 授课年级 医 18 药学 3 （全英文方 向） 授课章节 Chapter 10. Adrenergic Receptors and Drugs Affecting Adrenergic Neurotransmission 授课时间 2 课时 一、 教学目标：含知识目标、技能（能力）目标 3. 知识目标： （1） Get a general idea about adrenaline and adrenergic receptors; Understand the development history of drugs affecting adrenergic neurotransmission; （2） To master the chemical structures, drug design, structure-activity relationships, and mechanism of actions of major drugs affecting adrenergic neurotransmission; （3） Understand the synthesis and metabolism of major drugs affecting adrenergic neurotransmission 4. 技能（能力）目标：结合实验课程目标