Medicinal Chemistry

课程简介

/ Indicative Syllabus Basic chemical and biochemical concepts: Stereochemistry; chemistry of lipids, steroids, carbohydrates, amino acids, and nucleic acids; biochemistry of proteins, DNA and RNA, glycolipids and glycoproteins. Pharmacodynamics and pharmacokinetics: Drugs and medicinal chemist; the why and the wherefore - drug targets; proteins as drug targets; enzymes; receptors; receptor structure and signal transduction; nucleic acids as drug targets; pharmacokinetics and related topics; The process of drug development: -- 1 of 3 -- Screening and bioassays; the lead compounds; synthetic analogues; molecular modeling; pharmacodynamics; structure-activity relationships; physiochemical properties; drug design-optimizing PK properties; clinical testing Tools in drug discovery and development: Quantitative structure-activity relationships; combinatorial chemistry; Parallel synthesis. Selected topics in medicinal chemistry: Anti-cancer drugs: Cause of cancer; cell cycle, cancer chemotherapy; alkylating agents; anti- metabolites; intercalating agents; mitotic inhibitors; multidrug resistance; the mechanism of anti-cancer drugs and recent developments. Anti-viral drugs: How viruses reproduce; amantadine and analogs; the nucleoside analogs; the protease inhibitors; treatment of HIV by combination therapy; the development of zanamivir as anti-influenza drug; Drugs affecting cholinergic and adrenergic neurotransmitters: The neurotransmitters; cholinesterase inhibitors; cholinomimetics and Alzheimer's disease; anticholinergics; adrenoreceptors; selective a- and ß- blockers; Antibacterial agents The bacterial cell; mechanisms of antibacterial action; antibacterial agents which inhibit cell metabolism; antibacterial agents which inhibit cell wall synthesis; antibacterial agents which act on the plasma membrane structure; antibacterial agents which impair protein synthesis; antibacterial agents which act on nucleic acid transcription and replication; drug resistance The content of this subject is subject to change with reference to Graham L. Patrick’s book - An Introduction to Medicinal Chemistry.

目标

After taking this subject, students will have a systematic understanding of the basic chemical and biochemical basis of drug research and development in the pharmaceutical industry; the analytical skill in evaluate the benefits and limitations of therapeutic agents currently in use or understanding; and a stronger interest in the discipline of chemical technology and applied biology.

先修要求

ABB programme: Organic Chemistry I with Grade A- or above ASTC programme: Biochemistry or equivalent with Grade B+ or above, and Organic Chemistry I with Grade A- or above CT programme: Organic Chemistry II, and Biochemistry or equivalent with Grade B+ or above