課程資訊
課程名稱
藥物設計與開發
DRUG DESIGN AND DEVELOPMENT 
開課學期
97-2 
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
星期二5,6(12:20~14:10) 
上課地點
新302 
備註
本課程中文授課,使用英文教科書。外系所學生選修需經授課教師同意。
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/972drugdd 
課程簡介影片
 
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課程概述

1. General aspects: Optimization of lead compounds, Structure–activity relationship, Oral bioavailability, pharmacokinetics.
2. Antibiotics and antibiotic resistance
3. Aspirins and Nonsteroidal anti-inflammatory agents (NSAIDs)
4. Hormone analogues: (a) Oral contraceptives (e.g. mifepristone (RU486)) ; (b) Histamine H2 receptor antagonists (ranitidine).
5. Tyrosine kinase inhibitors as effective anti-cancer therapy
6. Protein drugs
7. Herbal medicine
8. DNA-interactive agents  

課程目標
 
課程要求
Requirement for students: Anyone who took the courses of Organic Chemistry and Biochemistry  
預期每週課後學習時數
 
Office Hours
 
指定閱讀
 
參考書目
Textbooks:
(a) “An introduction to Medicinal Chemistry”
by Graham L. Patrick (Oxford University Press) 3rd Edition ISNB 0199275009
(b) “The Organic Chemistry of Drug Design and Drug Action”
by Richard B. Silverman (Elsevier)

Reference Book
(c) “Drug Discovery: A History”
by Water Sneader (John Wiley)
 
評量方式
(僅供參考)
   
課程進度
週次
日期
單元主題
第1週
  General aspects
Provide basic terminology and concept, including optimization of lead compounds, structure–activity relationship, oral bioavailability, and pharmacokinetics 
第2週
  General Aspects-
Provide basic terminology and concept, including optimization of lead compounds, structure–activity relationship, oral bioavailability, and pharmacokinetics 
第3週
03/03  Antibiotics and antibiotic resistance-Describe the discovery of penicillins and our long-standing battles against bacteria 
第4週
03/10  Antibiotics and antibiotic resistance-Describe the discovery of penicillins and our long-standing battles against bacteria 
第5週
03/17  Aspirins and nonsteroidal anti-inflammatory agents (NSAIDs)-What happen about the sour success of selective cox-2 inhibitors? 
第7週
03/31  Aspirins and nonsteroidal anti-inflammatory agents (NSAIDs)-What happen about the sour success of selective cox-2 inhibitors? 
第8週
04/07  Tyrosine kinase inhibitors as effective anti-cancer therapy :There are 518 kinases encoded in the human genome, how are specific kinases inhibited for therapeutic development? 
第9週
04/14  期中考週 
第10週
04/21  Tyrosine kinase inhibitors as effective anti-cancer therapy : There are 518 kinases encoded in the human genome, how are specific kinases inhibited for therapeutic development?

(第一週分組報告 oral presentation 1) 
第11週
04/28  Hormone analogues as contraceptives and antiulcer agents : Describe the mode of action of (i) mifepristone (RU486) and (ii) histamine receptor antagonists (ranitidine). (第二週分組報告 oral presentation 2) 
第12週
05/05  Hormone analogues as contraceptives and antiulcer agents : Describe the mode of action of (i) mifepristone (RU486) and (ii) histamine receptor antagonists (ranitidine). (第三週分組報告 oral presentation 3) 
第13週
05/12  Targeting proteases: success, failures and future prospects : Historic review of ACE inhibitors (for the treatment of hypertension) and HIV protease inhibitors (for that of AIDS) (第四週分組報告 oral presentation 4) 
第14週
05/19  Targeting proteases: success, failures and future prospects : Historic review of ACE inhibitors (for the treatment of hypertension) and HIV protease inhibitors (for that of AIDS) (第五週分組報告 oral presentation 5) 
第15週
05/26  Protein drugs : Most of protein drugs are glycoproteins. Why are glycosylations so important? (第六週分組報告 oral presentation 6) 
第16週
06/02  Protein drugs : Most of protein drugs are glycoproteins. Why are glycosylations so important? (第七週分組報告 oral presentation 7) 
第17週
06/09  (Optional) Opium analgestics : Understand the mode of action associated with pain-killing and addition (第八週分組報告 oral presentation 8) 
第18週
06/16  期末考週