課程大綱

課程資訊

課程名稱

藥物設計與開發
Drug Design and Development

開課學期

100-2

授課對象

理學院化學系

授課教師

林俊宏

課號

Chem5058

課程識別碼

223 U2650

班次

學分

全/半年

半年

必/選修

選修

上課時間

星期二7,8(14:20~16:20)

上課地點

化217

備註

本課程中文授課,使用英文教科書。外系所學生選修須經授課老師同意。
限學士班三年級以上且限本系所學生(含輔系、雙修生)
總人數上限：60人

Ceiba 課程網頁

http://ceiba.ntu.edu.tw/1002Chem5058

課程簡介影片

核心能力關聯

核心能力與課程規劃關聯圖

課程大綱

為確保您我的權利,請尊重智慧財產權及不得非法影印

課程概述

1. General aspects : Provide basic terminology and concept, including optimization of lead compounds, structure–activity relationship, oral bioavailability, and pharmacokinetics
2. Antibiotics and antibiotic resistance : Describe the discovery of penicillins and our long-standing battles against bacteria
3. Aspirins and nonsteroidal anti-inflammatory agents (NSAIDs) : What happens about the sour success of selective COX-2 inhibitors?
4. Tyrosine kinase inhibitors as effective anti-cancer therapy : There are 518 kinases encoded in the human genome. Specific kinases are targeted for therapeutic development. Some of the examples and the strategies will be reviewed.
5. Antiulcer drugs : What are the successful stories of Tagamet™ and Zantac™, million-dollar-blockbusters?
6. Antiviral agents : Historic review of HIV protease and neuraminidase inhibitors
7. Case studies: Statins and ACE inhibitors : Historic review of Statins (for lowering cholesterol) and ACE inhibitors (for treatment of hypertension)
8. Successful stories of drug molecules: Development from bench to clinical use

Special features of this course:
(a) Course notes (課程講義 ~100 pages) are available.
(b) No written exam.
(c) Emphasis on the interaction between the teacher and students

課程目標

課程要求

Anyone is qualified for taking this course if either one of the conditions applies at least: (1) anyone who took or is taking the courses of Organic Chemistry and Biochemistry; (2) anyone who passed the course of Advanced Chemical Biology I or Advanced Chemical Biology II.

預期每週課後學習時數

Office Hours

指定閱讀

Textbook:
“An introduction to Medicinal Chemistry” by Graham L. Patrick (Oxford University Press), 4th Edition

參考書目

(a) “The Organic Chemistry of Drug Design and Drug Action” by Richard B.
Silverman (Elsevier)
(b) “Drug Discovery: A History” by Water Sneader (John Wiley)
(c) “Wilson and Gisvold’s Textbook of Organic Medicinal and Pharmaceutical
Chemistry” 11th Edition, by John H. Block and John M. Beale, Jr. (Lippincott
Williams & Wilkins)

評量方式
(僅供參考)

No.	項目	百分比	說明
1.	Oral presentation	100%	Oral presentations : All the students will be grouped into 7-8 groups. Each group will be assigned 1-2 papers for oral presentation (45 min power-point presentation). In addition, two students are scheduled to brief in each class and present the 5 best figures.

課程進度

週次	日期	單元主題
第0週	02/14	課程規定, 進度, 分組報告請看這裡
第1週	2/21	(1) 一般常識; General aspects : What is the common sense and knowledge in the business of drug discovery?
第2週	3/6	(2) 抗生素與抗藥性; Antibiotics and antibiotic resistance : beta-Lactams (e.g. penicillin) and Glycopeptoode (e.g. vancomycin)
第3週	3/13	(3)抗生素與抗藥性; Antibiotics and antibiotic resistance : Other antibiotics and types and mechanism of antibiotic resistances
第4週	3/20	(4)止痛藥; Aspirins and nonsteroidal anti-inflammatory agents (NSAIDs) : Aspirins and other nonsteroidal anti-inflammatory agents (NSAIDs)
第5週	3/27	(5) 止痛藥; Aspirins and nonsteroidal anti-inflammatory agents (NSAIDs) : Problems of Cyclooxygenase-2 (COX-2) inhibitors.
第6週	4/10	(6) 使用磷酸化酵素抑制物為新型抗癌藥物; Tyrosine kinase inhibitors as effective anti-cancer therapy : Covering mainly on the textbook; Kinase inhibitors against the Epidemal growth factor receptor (EGFR), Abelson tyrosine kinase, Cycline-dependet kinase (CDK).
第7週	4/17	(7) 使用磷酸化酵素抑制物為新型抗癌藥物; Tyrosine kinase inhibitors as effective anti-cancer therapy : Covering maninly on the review papers; Updated information about type I and type II inhibitors.
第8週	4/24	(8) 胃藥;Antiulcer drugs : Development of Cimetidine and Ranitidine (as H2 Antagonists)
第9週	5/1	(9) 胃藥;Antiulcer drugs : Development of Omeprazole and Esomeprazole (as proton pump inhibitors)
第10週	5/8	(10) 抗病毒藥物;Antiviral agents : Development of HIV protease inhibitors (e.g. Saquinivir, Ritonavir,…)
第11週	5/15	(11) 抗病毒藥物;Antiviral agents : Development of viral neuraminidase inhibitors (E.g. Relenza, Tamiflu, …)
第12週	5/22	(12) 降血脂及降血壓藥物; Case studies: Statins and ACE inhibitors : Story about Atorvastatin and Simvastatin (Cholesterol-lowering pills)
第13週	5/29	(13) 降血脂及降血壓藥物; Case studies: Statins and ACE inhibitors : Story about captopril, Enalapril and Lisinopril (Angiotensin-converting enzyme inhibitors)
第14週	6/5	(14) 成功案例（由實驗室到臨床）;Successful stories of drug molecules: Development from bench to clinical use : A personal story of Prof. Richard Silverman at Northwestern University
第15週	6/12	Student presentations
第16週	6/19	Student presentations