Define the medicinal chemistry,pharmacy,pharmaceutics and pharmacopoeia,the contents of pharmaceutical care;the drug discovery process,the drug design strategy,the drug targets and the bioassay,the SAR/SPKR/STR;ethical code for pharmaceut ical researchers,understand the regulations and laws related to drug administration. 2.教学重难点 The natural product-based drug discovery,the rational drug design by manipulating the physicochemical properties of the lead. targets(enzyme and receptor)structure and function,the receptor function,affinity and potency and efficacy,the mechanism of enzyme catalysis,the approaches to find a lead and structural optimization,the SAR,SPKR,STR,case studies for the natural product drug,receptor antagonist drug,receptor agonist drug,enzyme inhibitor drug. 3.教学内容 1. Drug discovery from natural products to master basic concepts:the definition of medicinal chemistry,the definition of natural products,drug target,the pharmacophore,the lead compounds,the drug-like properties. To have a general idea or understand:the history and evolution of medicinal chemistry,why are natural products important for drug discovery,the isolation and identification of natural products,case studies of several classic clinic drugs directly from natural origin or derived from natural products,the innovative drug discovery process,approaches to find a lead. 1.2 Drug design and relationship of functional groups to pharmacologic activity to master basic concepts:the definition of physicochemical properties,the definition of structure and activity relationship, structure and pharmacokinetics relationship,structure and toxicity relationship;the concept and measurement of Ionization, Lipophilicity,Hydrogen bonding,stereochemistry;the definition of bioisostere and classifications. to get a knowledge or understand:how the structures determine the physicochemical properties and how the physicochemical properties affect the ADMET?How to design a drug?The theory and the examples on the drug design:how to find a hit,SAR and lead,lead optimization,Structure Modification:Bioisostere. 1.3 Receptors as targets for drug discovery to master basic concepts:the drug targets,the receptor and its classification,the ligand,the structure and function of 4 major classes of drug receptors,the receptor interactions:affinity,potency,efficacy,the agonist,the antagonist,Determination of Affinity: the role of chemical bonding,the role of conformation,the role of stereochemistry.Define the medicinal chemistry, pharmacy, pharmaceutics and pharmacopoeia, the contents of pharmaceutical care; the drug discovery process, the drug design strategy, the drug targets and the bioassay, the SAR/SPKR/STR; ethical code for pharmaceutical researchers, understand the regulations and laws related to drug administration. 2.教学重难点 The natural product-based drug discovery, the rational drug design by manipulating the physicochemical properties of the lead, targets (enzyme and receptor) structure and function, the receptor function, affinity and potency and efficacy, the mechanism of enzyme catalysis, the approaches to find a lead and structural optimization, the SAR, SPKR, STR, case studies for the natural product drug, receptor antagonist drug, receptor agonist drug, enzyme inhibitor drug. 3.教学内容 1. Drug discovery from natural products to master basic concepts: the definition of medicinal chemistry, the definition of natural products, drug target, the pharmacophore, the lead compounds, the drug-like properties. To have a general idea or understand: the history and evolution of medicinal chemistry, why are natural products important for drug discovery, the isolation and identification of natural products, case studies of several classic clinic drugs directly from natural origin or derived from natural products, the innovative drug discovery process, approaches to find a lead. 1.2 Drug design and relationship of functional groups to pharmacologic activity to master basic concepts: the definition of physicochemical properties, the definition of structure and activity relationship, structure and pharmacokinetics relationship, structure and toxicity relationship; the concept and measurement of Ionization, Lipophilicity, Hydrogen bonding, stereochemistry; the definition of bioisostere and classifications. to get a knowledge or understand: how the structures determine the physicochemical properties and how the physicochemical properties affect the ADMET? How to design a drug? The theory and the examples on the drug design: how to find a hit, SAR and lead, lead optimization, Structure Modification: Bioisostere. 1.3 Receptors as targets for drug discovery to master basic concepts: the drug targets, the receptor and its classification, the ligand, the structure and function of 4 major classes of drug receptors, the receptor interactions: affinity, potency, efficacy, the agonist, the antagonist, Determination of Affinity: the role of chemical bonding, the role of conformation, the role of stereochemistry