Medicinal Chemistry 2012Autumn semester Some Important Concepts IUPACMedicinal

药物化学 Medicinal Chemistry 2012，Autumn semester

一、 药物化学中的一些概念 Some Important Concepts • IUPAC：Medicinal Chemistry is a chemistry-based discipline, involving aspects of biological, medical and pharmaceutical sciences. It is concerned with the invention, discovery, design, identification and preparation of biological active compounds, the study of their metabolism, the interpretation of their mode of action at the molecular level and the construction of structure-activity relationship (SAR), the relationships between chemical structure and pharmacological activity for a series of compounds.

二、 一些术语中英文对照 Contrast of English and Chinese Version of Specific terms • 构效关系(SAR)： Structure and Activity • • Relationship. 构性关系(SPR) ：Structure and Property Relationship. 药物分子设计(MDD)： Molecular Drug Design. 先导化合物(LC)：Lead Compound. 化学实体(NCE)：New Chemical Entities.

三、药物化学的四大任务 Four Main Tasks of Medicinal Chemistry I MDD Separation identification Structure modification SAR Develop new drug Medicament design III II SPR SAR Property Stability Molecular mechanism Design Metabolic process of side-effect Improvement Clinical use Pharmaceutical process Identification Impurity test Basic theory for Preclinical usage Determination Storage IV Synthesis

四、药物化学简史回顾 【早期实例】 Examples • Morphine: Analgesics • Quinine: Antimalarial • Atropine : Anticholinergic • Cocaine: Local Anesthetics

四、药物化学简史回顾 【现代实例】 SBDD HIV 蛋白酶抑制剂 • L-735524 Indinavi • Ro 31 -8959 Inviraser，Saquinavir

九、我国药化的发展状况 （二）方向 • MDD, SAR, Mechanism, Theory, CADD, • • Funding, New Methods and Biotechnics, Gene engineering, Lab and Center, LC from TCM. 非专利药的研发； 开发自主产权的新药。

药物化学部分相关期刊杂志 • • • 1. J. Med. Chem. ACS 2. J. Nat. Prod. ACS 3. Bioorg. Med. Chem. Lett. 4. Bioorg. Med. Chem. 5. ACS Chem. Bio. ACS 6. J. Am. Chem. Soc. ACS 7. J. Org. Chem. ACS 8. 中国药物化学杂志 9. 医药 业杂志 10. 各药学院校学报

Kindly Reminds • My Email address: mengge@mail. xjtu. edu. cn, • Tel: 82656327, • Office: Pharm Building 317, • Lab: Pharm Building 108.