The most prescribed antibiotic:quinolones and cephalosporins Combination use:cephalosporins along with lactamase inhibitors 7.2 Antifungal agents Master the most important antifungal drug is the triazole class,which target the fungal membrane ergosterol biosynthesis.Along this synthesis pathway,there are four drug target enzymes:the squalene oxidase,lanosterol,A14-reductase,A8,A7-isomerase.The 2nd most prescribed drug class is the polyene and the other widely used antifungal drug in the clinic is the Echinocandins;Update antifungal drug development. Structural feature of the azole drugs,specific mechanism of action,selectivity of these drugs. 7.3 Antimycobacterial agents Master the four first-line anti-TB drugs:isoniazid,ethambutol,Pyrazinamide,Rifamycin.Understand their mechanism of action, recognize the molecules when provided. Updated anti-TB drugs developed after 2000:the nitro-imidazole type,Bedaquiline The second line anti-TB drug:Streptomycin and the 4th generation quinolones 7.4 Cancer and chemotherapy Cancer chemotherapy drugtype:(1)alkylating agents;(2)Organoplatinum complexes;(3)Antimetabolites,(4)DNA Polymerase/DNA Chain Elongation Inhibitors;(5)Mitosis Inhibitor taxol;(6)Kinase inhibitors;(7)epigenetic drugs. Students are required to master the major drugs in each class,drug pharmacophore,mechanism of action,side effects. 7.5 Antiviral agents Master drugs used for the treatment of influenza (Neuramidase inhibitor),HIV,HCV; Conventional Nucleoside Analogs,specific purine and pyrimidine analogs as anti-viral drugs; 1.Nucleoside Reverse Transcriptase Inhibitor(NRTIs)as anti-HIV drugs;specific drugs:AZT,ABC,et al;(2)protease inhibitors as anti-viral drugs;(3)Integrase inhibitors as anti-viral drugs.Specific drugs include:Elvitegravir,Dolutegravir, Bictegravir. HCV drug development after 2010:Nonstructural protein 5B (NS5B):NS5B;NS3/4A Protease inhibitors;specific drugs: sofosbuvir,Telaprevir,Bocsprevir (三)课程目标与毕业要求、课程内容的对应关系 表1：课程目标与课程内容、毕业要求的对应关系表
The most prescribed antibiotic: quinolones and cephalosporins. Combination use: cephalosporins along with lactamase inhibitors 7.2 Antifungal agents Master the most important antifungal drug is the triazole class, which target the fungal membrane ergosterol biosynthesis. Along this synthesis pathway, there are four drug target enzymes: the squalene oxidase, lanosterol, Δ14 -reductase, Δ8 , Δ7 -isomerase. The 2 nd most prescribed drug class is the polyene and the other widely used antifungal drug in the clinic is the Echinocandins; Update antifungal drug development. Structural feature of the azole drugs, specific mechanism of action, selectivity of these drugs. 7.3 Antimycobacterial agents Master the four first-line anti-TB drugs: isoniazid, ethambutol, Pyrazinamide, Rifamycin. Understand their mechanism of action, recognize the molecules when provided. Updated anti-TB drugs developed after 2000: the nitro-imidazole type, Bedaquiline The second line anti-TB drug: Streptomycin and the 4th generation quinolones 7.4 Cancer and chemotherapy Cancer chemotherapy drug type: (1) alkylating agents; (2) Organoplatinum complexes; (3) Antimetabolites; (4) DNA Polymerase/DNA Chain Elongation Inhibitors; (5) Mitosis Inhibitor taxol; (6) Kinase inhibitors; (7) epigenetic drugs. Students are required to master the major drugs in each class, drug pharmacophore, mechanism of action, side effects. 7.5 Antiviral agents Master drugs used for the treatment of influenza (Neuramidase inhibitor), HIV, HCV; Conventional Nucleoside Analogs, specific purine and pyrimidine analogs as anti-viral drugs; 1. Nucleoside Reverse Transcriptase Inhibitor (NRTIs) as anti-HIV drugs; specific drugs: AZT, ABC, et al; (2) protease inhibitors as anti-viral drugs; (3) Integrase inhibitors as anti-viral drugs. Specific drugs include: Elvitegravir, Dolutegravir, Bictegravir. HCV drug development after 2010: Nonstructural protein 5B (NS5B): NS5B; NS3/4A Protease inhibitors; specific drugs: sofosbuvir, Telaprevir, Bocsprevir （三）课程目标与毕业要求、课程内容的对应关系 表 1：课程目标与课程内容、毕业要求的对应关系表
课程目标 课程子目标 对应课程内容 对应单业要求 The principals of medicinal chemistry, terms,basic concepts. Students are expected to understand and Objectivel Knowledge learning Drug pharmacophores,mechanism of remember specific first-line drugs in each action,metabolism,synthetic method,side disease area effects Objective Nomenclatures,professional words in the Improved professional English reading and 2 Language learning textbook understanding level Objective Critical thinking and Most updated drug development in major Deep-learning,problem solving ability 3 problem solving pharms development 三、教学内容 Section 1.Principles of drug discovery 1教学目标
课程目标 课程子目标 对应课程内容 对应毕业要求 Objective1 Knowledge learning The principals of medicinal chemistry, terms, basic concepts. Drug pharmacophores, mechanism of action, metabolism, synthetic method, side effects Students are expected to understand and remember specific first-line drugs in each disease area Objective 2 Language learning Nomenclatures, professional words in the textbook Improved professional English reading and understanding level Objective 3 Critical thinking and problem solving Most updated drug development in major pharms Deep-learning, problem solving ability development 三、教学内容 Section 1. Principles of drug discovery 1.教学目标
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
the students are required to get a knowledge or understand:how to define and determine Potency and Efficacy of receptors, agonist types,dose-response curve,Orthosteric and Allosteric Antagonist,voltage-gated and ligand-gated ion-channels,GPCR, transmembrane catalytic receptor,cytoplasmic or nuclear receptor;GPCR Signal Transduction;the GPCR Assays in the Lab;case study of several receptor antagonist or agonist as therapeutic agents. 1.4 Drug discovery through enzyme inhibition to master basic concepts:enzymes as catalytic proteins and general concepts of enzyme inhibitors and their rational design into drugs,the structure and function of enzymes,the enzyme kinetics,covalent catalysis,Lineweaver-Burk plot of 1/v versus 1/[S]and the key parameters,enzyme inhibitor design strategy,irreversible enzyme inhibitor to get a knowledge or understand:the naming of enzymes,the mechanism of the enzyme catalysis,Enzyme Inhibitors: Competitive and noncompetitive,reversible and irreversible,case study of typical enzyme inhibitor discovery and development, mechanism and evolution of covalent enzyme inhibitors. 4.教学方法 (1)Teaching method:Relevant concepts and theoretical framework (2)Discussion method:The use of heuristic teaching. 5.教学评价 Quick summary test and discuss selected frequently asked questions. Section 2.Drugs receptors affecting neurotransmission and enzymes as catalytic receptors 2.1 Drugs affecting cholinergic neurotransmission Get a general idea about neurotransmitters and associated neuropsychiatric disease;Get a general idea about acetylcholine and its functions and neurochemistry,and the distribution,structures and functions of cholinergic receptors.Get a general idea about Alzheimer disease. Understand the development history of cholinergic drugs
the students are required to get a knowledge or understand: how to define and determine Potency and Efficacy of receptors, agonist types, dose-response curve, Orthosteric and Allosteric Antagonist, voltage-gated and ligand-gated ion-channels, GPCR, transmembrane catalytic receptor, cytoplasmic or nuclear receptor;GPCR Signal Transduction; the GPCR Assays in the Lab; case study of several receptor antagonist or agonist as therapeutic agents. 1.4 Drug discovery through enzyme inhibition to master basic concepts: enzymes as catalytic proteins and general concepts of enzyme inhibitors and their rational design into drugs, the structure and function of enzymes, the enzyme kinetics, covalent catalysis, Lineweaver-Burk plot of 1/v versus 1/[S] and the key parameters, enzyme inhibitor design strategy, irreversible enzyme inhibitor to get a knowledge or understand: the naming of enzymes, the mechanism of the enzyme catalysis, Enzyme Inhibitors: Competitive and noncompetitive, reversible and irreversible, case study of typical enzyme inhibitor discovery and development, mechanism and evolution of covalent enzyme inhibitors. 4.教学方法 (1) Teaching method: Relevant concepts and theoretical framework. (2) Discussion method: The use of heuristic teaching. 5.教学评价 Quick summary test and discuss selected frequently asked questions. Section 2. Drugs receptors affecting neurotransmission and enzymes as catalytic receptors 2.1 Drugs affecting cholinergic neurotransmission Get a general idea about neurotransmitters and associated neuropsychiatric disease; Get a general idea about acetylcholine and its functions and neurochemistry, and the distribution, structures and functions of cholinergic receptors. Get a general idea about Alzheimer disease. Understand the development history of cholinergic drugs