{"ModuleCode":"PR3101","ModuleTitle":"Principles Of Medicinal Chemistry","Department":"Pharmacy","ModuleDescription":"Learning objectives: To impart an understanding of drugs as chemical entities whose biological activities are dependent on chemical structure and physicochemical properties. To have an understanding of the following properties/characteristics of a drug molecule and how they may influence activity: solubility, ionisation characteristics, lipophilicity, stereochemistry, metabolism. To be able to analyse data to provide a preliminary analysis of structure activity relationship. Major topics: Basic principles of drug design. Medicinal chemistry of selected groups of compounds will be discussed to emphasize relationships between structure, physicochemical properties and the molecular basis of drug action, where appropriate.Target students: Pharmacy Year Three and Applied Chemistry (Drug Option)","ModuleCredit":"4","Workload":"2.5-0.5-2-1-4","Prerequisite":"PR1101","ExamDate":"2015-12-02T13:00+0800","ExamDuration":"P2H","ExamVenue":"MPSH2-A","Types":["Module"],"Lecturers":["Dymock, Brian William"],"IVLE":[{"Announcements":null,"Forums":[],"Workbins":[],"Webcasts":[],"Gradebooks":[],"Polls":[],"Multimedia":[],"LessonPlan":[],"ID":"91025903-b43c-4757-9ba4-fe86324d5593","CourseLevel":"1","CourseCode":"PR3101","CourseName":"PRINCIPLES OF MEDICINAL CHEMISTRY","CourseDepartment":"","CourseSemester":"Semester 1","CourseAcadYear":"2015/2016","CourseOpenDate":"/Date(1435052280000+0800)/","CourseOpenDate_js":"2015-06-23T17:38:00","CourseCloseDate":"/Date(1449244800000+0800)/","CourseCloseDate_js":"2015-12-05T00:00:00","CourseMC":"0","isActive":"Y","Permission":"S","Creator":{"UserID":null,"Name":"Dymock, Brian William","Email":null,"Title":null,"UserGuid":"e1c3c14e-9894-4772-b840-9d028ae93962","AccountType":null},"hasGradebookItems":false,"hasTimetableItems":true,"hasGroupsItems":false,"hasClassGroupsForSignUp":false,"hasGuestRosterItems":false,"hasClassRosterItems":false,"hasWeblinkItems":false,"hasLecturerItems":true,"hasDescriptionItems":true,"hasReadingItems":false,"hasAnnouncementItems":false,"hasProjectGroupItems":false,"hasProjectGroupsForSignUp":false,"hasConsultationItems":false,"hasConsultationSlotsForSignUp":false,"hasLessonPlanItems":false,"Badge":0,"BadgeAnnouncement":0,"WebLinks":[],"Lecturers":[{"ID":"4a23451f-c5ae-4538-95e1-556c6fe2c4f1","User":{"UserID":null,"Name":"Dymock, Brian William","Email":null,"Title":null,"UserGuid":"e1c3c14e-9894-4772-b840-9d028ae93962","AccountType":null},"Role":"Lecturer ","Order":1,"ConsultHrs":null}],"Descriptions":[{"ID":"1e5f053b-8835-4692-be49-41f07234cfff","Title":"Learning Outcomes","Description":"At the end of the module you will learn about
\r\n \r\n
\r\n\t- The importance of targeted drug design in modern pharmacy
\r\n\t- How to discover, design and optimize a drug molecule
\r\n\t- Development of drugs into the clinic
\r\n\t- Case studies of some prominent drugs
\r\n
\r\nMore specific objectives are:
\r\n \r\n\r\n\t\r\n\t\t\r\n\t\t\t\r\n\t\t\t\r\n\t\t\t\t- To understand drugs as chemical entities whose biological activities are dependent on the chemical structure and physicochemical properties.
\r\n\t\t\t\t- To understand how various characteristics of drugs (solubility, ionization, lipophilicity, stereochemistry, metabolism) affect activity.
\r\n\t\t\t\t- To gain knowledge on the common methods used in design and synthesis of drugs
\r\n\t\t\t\t- To understand the phases of the drug discovery process, the basics of patenting new molecules and an introduction to the drug development process
\r\n\t\t\t \r\n\t\t\t | \r\n\t\t
\r\n\t\r\n
\r\n","Order":1},{"ID":"2e5f053b-8835-4692-be49-41f07234cfff","Title":"Prerequisites","Description":"PR1101 ","Order":2},{"ID":"3e5f053b-8835-4692-be49-41f07234cfff","Title":"Teaching Modes","Description":"The module will be delivered by lectures, tutorials and a computational practical ('dry' lab). The CA component will include class mini-quizzes and a test. Subject to changes.","Order":3},{"ID":"5e5f053b-8835-4692-be49-41f07234cfff","Title":"Synopsis","Description":"The aim of this module is to give students a better understanding of the chemical, biochemical and mechanistic considerations underlying drug design and action. The science involved in the discovery, development, identification and the interpretation of the mode of action of biologically active compounds at the molecular level is essential for pharmacists. A pharmacist is an experts in drugs and hence must know where drugs come from and how they work. Medicinal chemistry helps you to understand the drug molecule from the stand point of the functional groups present and its stereochemistry. The emphasis here will be placed on the drug substance itself (API) but not necessarily restricted to it. E.g. we will look at processes in drug discovery and some aspects of drug development and formulation. Medicinal chemistry is a combination of sciences at the interface of chemistry and life sciences hence the coverage will be fairly broad and interdisciplinary, with a focus on detailed molecular aspects.
\r\n
\r\nThe topics that will be covered in the module are listed as follows:
\r\nOverviews (brief and covered as reminders)
\r\n \r\n\r\n\t- Overview of the Drug Discovery Process – what is medicinal chemistry?
\r\n\t- Overview of types of drug targets (receptors, enzymes, ion channels, other intracellular targets)
\r\n\t- Overview of protein structure
\r\n
\r\nDrug Discovery (introductory)
\r\n \r\n\r\n\t- Drug Discovery: finding a lead compound
\r\n\t- Methods of screening, assay types, what is an IC50, enzyme kinetics
\r\n\t- Hit to Lead process, nomenclature, objectives
\r\n
\r\nDrug Design (in depth)
\r\n \r\n\r\n\t- Drug Design: optimizing interaction between a ligand and its biological target
\r\n\t- Drug Design: optimizing access of a drug to its target; Molecular and Physical Properties of Drugs (‘physicochemical properties’, use of bioisosteres, etc)
\r\n\t- Synthesis in medicinal chemistry (combinatorial, parallel, medchem strategies, scale-up for the clinic).
\r\n\t- Structure-based design
\r\n\t- Molecular Modelling
\r\n\t- QSAR
\r\n
\r\nDrug Development (introductory)
\r\n \r\n\r\n\t- Drug Development Topics: preclinical to clinical (what are the objectives)
\r\n\t- Pro-drugs, formulation, toxicity
\r\n\t- Introduction to Patents – what are they and why do we need them?
\r\n
\r\nCase Studies (in depth where relevant to learning objectives)
\r\n \r\n\r\n\t- Antibacterial
\r\n\t- Anticancer
\r\n\t- Antivirals
\r\n\t- CNS/pain
\r\n
\r\n","Order":5},{"ID":"6e5f053b-8835-4692-be49-41f07234cfff","Title":"Syllabus","Description":"\r\n\t\r\n\t\t\r\n\t\t\t\r\n\t\t\t\r\n\t\t\t\t- Drug-like properties
\r\n\t\t\t\t- Lead optimization strategies: Functional groups, bioisosteres, conformational restriction, homologation.
\r\n\t\t\t\t- Optimizing a lead : Metabolism and structure modification strategies to reduce metabolism
\r\n\t\t\t\t- Optimizing a lead: Prodrugs- design and applications
\r\n\t\t\t\t- Computer aided drug design: Introduction to Structure-and Ligand-based design. In silico ADMET
\r\n\t\t\t\t- Drug synthesis: Chemical transformations commonly used in drug synthesis (minor introduction)
\r\n\t\t\t\t- Introduction to patents: why patent a molecule, how a patent is structured
\r\n\t\t\t\t- Introduction of Drug Development: different phases, skills/knowledge required at each stage
\r\n\t\t\t \r\n\t\t\t | \r\n\t\t
\r\n\t\r\n
\r\n","Order":6},{"ID":"c23b98a1-3343-42d0-a8b3-91734c3a661c","Title":"Workload","Description":"2.5-0.5-2-1-4
Workload Components : A-B-C-D-E \r\n
A: no. of lecture hours per week \r\n
B: no. of tutorial hours per week \r\n
C: no. of lab hours per week \r\n
D: no. of hours for projects, assignments, fieldwork etc per week \r\n
E: no. of hours for preparatory work by a student per week","Order":9}],"ReadingFormatted":[],"ReadingUnformatted":[]}],"Timetable":[{"ClassNo":"SB1","LessonType":"Laboratory","WeekText":"Every Week","DayText":"Tuesday","StartTime":"1400","EndTime":"1700","Venue":"S14-04Lab"},{"ClassNo":"SB2","LessonType":"Laboratory","WeekText":"Every Week","DayText":"Friday","StartTime":"1400","EndTime":"1700","Venue":"S14-04Lab"},{"ClassNo":"SL1","LessonType":"Lecture","WeekText":"Every Week","DayText":"Monday","StartTime":"1200","EndTime":"1400","Venue":"LT33"},{"ClassNo":"SL1","LessonType":"Lecture","WeekText":"Every Week","DayText":"Thursday","StartTime":"1200","EndTime":"1400","Venue":"LT33"}],"CorsBiddingStats":[{"AcadYear":"2005/2006","Semester":"1","Round":"1A","Group":"Lecture Sl1","Quota":"20","Bidders":"3","LowestBid":"1","LowestSuccessfulBid":"1","HighestBid":"500","Faculty":"Science","StudentAcctType":"Returning Students [P]"},{"AcadYear":"2005/2006","Semester":"1","Round":"1B","Group":"Lecture Sl1","Quota":"17","Bidders":"1","LowestBid":"1","LowestSuccessfulBid":"1","HighestBid":"1","Faculty":"Science","StudentAcctType":"Returning Students [P]"},{"AcadYear":"2005/2006","Semester":"1","Round":"1C","Group":"Lecture Sl1","Quota":"16","Bidders":"16","LowestBid":"1","LowestSuccessfulBid":"1","HighestBid":"1000","Faculty":"Science","StudentAcctType":"Returning Students [P]"}],"LecturePeriods":["Monday Afternoon","Thursday Afternoon"],"TutorialPeriods":["Tuesday Afternoon","Friday Afternoon"]}